781649-86-3

Usage

Uses

Used in Pharmaceutical Industry:
1-Piperidinecarboxylic acid, 4-[(2-amino-3-pyridinyl)amino]-, 1,1-dimethylethyl ester is used as a therapeutic agent for the treatment of erectile dysfunction and benign prostatic hyperplasia. It is utilized for its ability to increase blood flow to the penis, leading to improved erections and overall sexual function in affected individuals.
Used in Men's Health Applications:
Tadalafil serves as a crucial medication in men's health, specifically addressing erectile dysfunction. It helps men achieve and maintain erections sufficient for sexual activity, thereby improving their quality of life and sexual satisfaction.
Used in Urological Treatments:
In the field of urology, tadalafil is employed for the management of benign prostatic hyperplasia, a condition that affects aging men and can cause urinary symptoms and complications. By improving blood flow, tadalafil can alleviate some of the symptoms associated with this condition.

InChI:InChI=1/C15H24N4O2/c1-15(2,3)21-14(20)19-9-6-11(7-10-19)18-12-5-4-8-17-13(12)16/h4-5,8,11,18H,6-7,9-10H2,1-3H3,(H2,16,17)

Upstream product

• 452-58-4 2,3-Diaminopyridine 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 6298-19-7 2-chloro-3-aminopyridine 
• 1155016-22-0 tert-butyl 4-(2-chloropyridin-3-ylamino)piperidine-1-carboxylate 
• 54231-35-5 3-fuoro-2-nitropyridine 
• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 

Downstream Products

• 781649-87-4 tert-butyl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]-pyridin-1-yl)piperidine-1-carboxylate 

Relevant academic research and scientific papers

Synthesis of a dual carbon-14-labeled calcitonin gene-related peptide receptor antagonist for use in a human absorption–distribution–metabolism–elimination study

Oral calcitonin gene-related peptide (CGRP) receptor antagonists have been shown to be effective in the acute and preventive treatment of migraine. CGRP receptor antagonists offer safety advantages over triptans because they are not active vasoconstrictors, which reduces cardiovascular risks. Bristol Myers Squibb discovered a high affinity CGRP receptor antagonist BMS-927711 for the treatment of migraine now FDA approved as Nurtec ODT (rimegepant). Dual-labeled [14C]-BMS-927711 was prepared and used in a human absorption–distribution–metabolism–elimination (ADME) study. A dual-labeled analog of BMS-927711 was required to fully track the compound's metabolic transformation. The carbon-14-labeled synthesis of both right side and left side portions of [14C]-BMS-927711 is described.

HETEROCYCLIC COMPOUND, APPLICATION THEREOF, AND COMPOSITION CONTAINING SAME

A heterocyclic compound represented by formula XI, a pharmaceutically acceptable salt, a solvate, or a solvate of a pharmaceutically acceptable salt thereof, use thereof, and a composition containing the same. The compound is novel in structure and has good STAT5 inhibitory activity.

1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to 1,3,4-oxadiazole derivative compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a use thereof in preparation of a medicament, a pharmaceutical composition comprising the same, a therapeutic method using the composition, and a method for preparing the same, and the 1,3,4-oxadiazole derivative compounds are represented by a following chemical formula (I).

Development of two complementary syntheses for a privileged cgrp receptor antagonist substructure

1-(Piperidin-4-yl)-1H-imidazo[4,5-b]pyridin-2(3H)-one (1) is a privileged substructure found in >1000 unique CGRP receptor antagonists. Two practical and efficient syntheses of 1 are described from complementary starting materials. One route features a ch

INHIBITORS OF PI3K-DELTA AND METHODS OF THEIR USE AND MANUFACTURE

The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.

AMIDE-SUBSTITUTED ARYL PIPERIDINES

Amide-substituted aryl piperidines derivatives of the following Formulas are provided:(Formulas), in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache, such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.

BIARYL KETONE-SUBSTITUTED PIPERIDINES

Biaryl ketone-substituted piperidines of the following Formulas are provided:, and in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.

CONSTRAINED COMPOUNDS AS CGRP-RECEPTOR ANTAGONISTS

The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

HETEROCYCLIC BENZODIAZEPINE CGRP RECEPTOR ANTAGONISTS

Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

CGRP RECEPTOR ANTAGONISTS

Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache