247034-88-4

Upstream product

• 25437-94-9 ethyl 4-(4-hydroxypiperidin-1-yl)benzoate 
• 1158186-69-6 ethyl 4-(4-azidopiperidin-1-yl)benzoate 
• 1158186-68-5 ethyl 4-(4-((methylsulfonyl)oxy)piperidin-1-yl)benzoate 
• 13035-19-3 4-aminopiperidine 
• 451-46-7 4-fluorobenzoic acid ethyl ester 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 247034-87-3 ethyl 4-(4-phthalimidopiperidin-1-yl)benzoate 

Downstream Products

• 883727-00-2 ethyl 4-[4-[3-{4-(tert-butoxycarbonylamino)butyl}thioureido]piperidin-1-yl]benzoate 
• 329280-10-6 4-tert-butoxycarbonylamino-1-(4-ethoxycarbonyl-phenyl)piperidine 
• 247035-10-5 ethyl 4-[4-[3-{2-(tert-butoxycarbonylamino)ethyl}thioureido]piperidin-1-yl]benzoate 
• 247034-90-8 4-{4-(Pyrimidin-2-ylamino)piperidin-1-yl}benzoic acid 
• 247033-64-3 (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-ylamino)piperidin-1-yl}benzoylamino]propionic acid 
• 247033-63-2 tert-butyl (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-ylamino)piperidin-1-yl}benzoylamino]propionate 
• 247035-04-7 4-[4-{(tert-butoxycarbonyl)amino}piperidin-1-yl]benzoic acid 
• 883726-98-5 4-{4-(4,5-dihydro-1H-imidazol-2-ylamino)piperidin-1-yl}benzoic acid 
• 247035-09-2 ethyl 4-{4-(4,5-dihydro-1H-imidazol-2-ylamino)piperidin-1-yl}benzoate 
• 883727-01-3 4-{4-(4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-ylamino)piperidin-1-yl}benzoic acid 
• 247035-13-8 ethyl 4-{4-(4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-ylamino)piperidin-1-yl}benzoate 
• 324781-26-2 (2S)-hydroxy-3-[4-{4-(pyrimidin-2-ylamino)-piperidin-1-yl}benzoylamino]propionic acid 
• 324781-24-0 t-butyl (2S)-hydroxy-3-[4-{4-(pyrimidin-2-ylamino)-piperidin-1-yl}benzoylamino]propionate 
• 247035-06-9 tert-butyl 3-{4-(4-aminopiperidin-1-yl)benzoylamino}-(2S)-(benzenesulfonylamino)propionate 

Relevant academic research and scientific papers

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.

PROSTAGLANDIN D SYNTHASE INHIBITORY PIPERIDINE COMPOUNDS

The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.

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.

PIPERAZINE COMPOUND HAVING A PGDS INHIBITORY EFFECT

The present invention provides a piperazine compound represented by Formula (I) or a salt thereof, wherein X represents CH or an N atom; R1 represents C1-6 alkyl; R2 represents C1-6 alkyl that may have one or more substituents, C2-6 alkenyl that may have one or more substituents, -(C=O)-N(R3) (R4), or -(C=O)-OR5, R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents; or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; and R5 represents hydrogen or C1-6 alkyl that may have one or more substituents or aralkyl.

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.

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.

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.