25437-94-9

Upstream product

• 5382-16-1 4-HYDROXYPIPERIDINE 
• 451-46-7 4-fluorobenzoic acid ethyl ester 

Downstream Products

• 553672-07-4 4-(4-Hydroxy-1-piperidinyl)benzoic acid monohydrochloride 
• 718632-62-3 ethyl 4-(4-fluoropiperidin-1-yl)benzoate 
• 1246249-44-4 3-(1-(4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl)piperidin-4-yl)-1,1-dimethylurea 
• 1246249-43-3 2-[4-(4-aminopiperidin-1-yl)phenyl]-5,7-dimethoxyquinazolin-4(3H)-one 
• 1246249-42-2 N-{1-[4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]piperidin-4-yl}methanesulfonamide 
• 1246249-38-6 N-{1-[4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]piperidin-4-yl}acetamide 
• 247034-04-4 tert-butyl (2S)-benzenesulfonylamino-3-[4-{4-(4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-ylamino)piperidin-1-yl}benzoylamino]propionate 
• 883726-99-6 tert-butyl (2S)-benzenesulfonylamino-3-[4-{4-(4,5-dihydro-1H-imidazol-2-ylamino)piperidin-1-yl}benzoylamino]propionate 
• 247035-05-8 tert-butyl (2S)-benzenesulfonylamino-3-[4-[4-{(tert-butoxycarbonyl)amino}piperidin-1-yl]benzoylamino]propionate 
• 247033-86-9 tert-butyl (2S)-benzenesulfonylamino-3-{4-(4-guanidinopiperidin-1-yl)benzoylamino}propionate 
• 324781-29-5 t-butyl (2S)-t-butoxy-4-[4-{4-(pyrimidin-2-ylamino)piperidin-1-yl}benzoylamino]butyrate 
• 883727-00-2 ethyl 4-[4-[3-{4-(tert-butoxycarbonylamino)butyl}thioureido]piperidin-1-yl]benzoate 
• 247035-06-9 tert-butyl 3-{4-(4-aminopiperidin-1-yl)benzoylamino}-(2S)-(benzenesulfonylamino)propionate 
• 324781-24-0 t-butyl (2S)-hydroxy-3-[4-{4-(pyrimidin-2-ylamino)-piperidin-1-yl}benzoylamino]propionate 

Relevant academic research and scientific papers

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "tail Switching" Strategy on a Piperazinyl Azetidine Skeleton

Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological co

Anti-inflammatory agents

Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.

POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS

Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds,

Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part 1: Design and synthesis of a lead compound exhibiting αvβ3/ αIIbβ3 dual antagonistic activity

In order to generate novel compounds with integrin α vβ3-antagonistic activity together with antiplatelet activity, tricyclic pharmacophore-based molecules were designed and synthesized. Although piperazine-containing compounds initially prepared were selective αIIbβ3 antagonists, replacement of piperazine with piperidine furnished a potent αvβ3/ αIIbβ3 dual antagonist. Structure-activity relationship (SAR) studies provided clues for further development of tricyclic pharmacophore-based integrin antagonists.

Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part 2: Synthesis of potent αvβ3/αIIbβ3 dual antagonists

We synthesized 4-aminopiperidine derivatives of our prototype integrin αvβ3 antagonist 1 in an attempt to increase the activity and water solubility. Introduction of one or two hydrophilic moieties into the central aromatic ring and/or the benzene ring at the C-terminus of 1 increased water solubility and enhanced inhibition of cell adhesion. The results of a structure-activity relationships (SAR) study indicated that the torsion angle between the central aromatic ring and the piperidine ring, and the acidity at the sulfonamide moiety, might be important for αvβ 3 receptor binding activity. Some of these compounds are novel and potent αvβ3/αIIbβ 3 dual antagonists with acceptable water solubility and a satisfactory early absorption, distribution, metabolism, excretion, and toxicity (ADMET) profile.

SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS

Compounds represented by formula (Ia) or (lb) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disor

PYRAZOLOPYRIMIDINONE DERIVATIVES HAVING PDE7?INHIBITORY ACTIVITY

Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): and the following general formula (IA') or (IB'): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds have the action of selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, they are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.

Aminopiperidine derivates as integrin αvβ3 antagonists

An objective of the present invention is to provide compounds having integrin αvβ3antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2or the like; X and Z represent CH or a nitrogen atom; R7and R8represent alkyl, halogen or the like; Q represents >C═O, >CH2or the like; R9represents H, alkyl, aralkyl or the like; R10represents H, alkynyl or the like; R11represents H, substituted amino or the like; R12represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.