cas 249296-44-4, Varenicline | Articles data

Articles about 249296-44-4Total 14 be found

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Varenicline synthesis method
The present invention relates to a process for the preparation of varenicline or a pharmaceutically acceptable salt thereof. The invention also relates to an intermediate compound useful in the process and the preparation of such intermediate compound.
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Paragraph 0024; 0036

(2021/07/31)

Cocrystal of varenicline and oxalic acid, pharmaceutical composition thereof, and methods of use thereof
Provided is a cocrystal of varenicline and oxalic acid. In particular, provided is a cocrystal of varenicline and oxalic acid of formula (I) having a molar ratio of varenicline to oxalic acid of 1:1.5. Also provided is a process for preparing the cocrystal, a pharmaceutical composition containing the cocrystal and a method of using the cocrystal and pharmaceutical composition, such as for reducing nicotine addiction or tobacco use.
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(2021/06/23)

IMPROVED PROCESS FOR THE PREPARATION OF SUBSTITUTED QUINOXALINES
The present invention is directed to an improved process for the preparation of substituted quinoxalines by cyclization of the corresponding dianiline in the presence of ion exchange resin.
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Page/Page column 18

(2011/07/30)

HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY
Provided herein is an impurity of varenicline, 6-methyl-5,8,14-triazatetracyclo[l 0.3.1.02'n,04'9]hexadeca-2(l l),3,5,7,9-pentaene (methylvarenicline) impurity, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity.
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Page/Page column 20-21

(2011/10/05)

An efficient synthesis of varenicline
Synthesis of varenicline the antismoking drug has been achieved in six steps with 10% overall yield. A Diels-Alder reaction, oxidative cleavage of an olefin and reductive amination remain as key steps in the synthesis.
Pasikanti, Srinivas,Srinivasa Reddy,Venkatesham,Dubey,Iqbal, Javed,Das, Parthasarathi
experimental part
p. 151 - 152
(2010/03/03)

SOLID STATES FORMS OF VARENICLINE SALTS AND PROCESSES FOR PREPARATION THEREOF
Salts and crystalline forms of several salts of Varenicline, i.e., Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, methods of preparing the solid states of Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, and processes for preparing Varenicline base from those Varenicline salts are provided.
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Page/Page column 4

(2010/12/31)

PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien- 10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the pressence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2- trifluoro-ethanone.
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Page/Page column 18-19

(2010/04/06)

VARENICLINE TOSYLATE, AN INTERMEDIATE IN THE PREPARATION PROCESS OF VARENICLINE L-TARTRATE
Crystalline forms of Varenicline Tosylate, processes for preparing those crystalline forms of Varenicline Tosylate, and processes for obtaining high purity Varenicline base using Varenicline Tosylate are provided.
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Page/Page column 25

(2009/12/27)

A NEW POLYMORPHIC FORM OF A PYRAZINO[2,3-h][3] BENZAZEPINE DERIVATIVE
The invention relates generally to a crystalline polymorphic form of 7, 8, 9, 10-tetrahydro-6, 10-methano-6H-pyrazino[2, 3-h][3] benzazepine, varenicline base, i.e. a hydrate of varenicline base, designated herein as Form II, and to a method for preparing and obtaining the same.
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Page/Page column 7

(2009/10/09)

PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF
The invention provides an improved process for the preparation and purification of Varenicline and intermediates for the preparation of Varenicline.
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Page/Page column 11

(2009/12/28)

POLYMORPHS OF NICOTINIC INTERMEDIATES
Crystalline forms of compounds II, III and IV and processes to produce them are provided.
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Page/Page column 12-13

(2008/12/05)

VARENICLINE STANDARDS AND IMPURITY CONTROLS
The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamine mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than O ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.
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Page/Page column 10

(2008/06/13)

3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation
3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation.
Coe, Jotham W.,Brooks, Paige R.,Wirtz, Michael C.,Bashore, Crystal G.,Bianco, Krista E.,Vetelino, Michael G.,Arnold, Eric P.,Lebel, Lorraine A.,Fox, Carol B.,Tingley III, F. David,Schulz, David W.,Davis, Thomas I.,Sands, Steven B.,Mansbach, Robert S.,Rollema, Hans,O'Neill, Brian T.
p. 4889 - 4897
(2008/12/23)

Pharmaceutical composition and method of modulating cholinergic function in a mammal
A pharmaceutical composition and method of modulating cholinergic function in a mammal comprising administration of a NRPA compound or a pharmaceutically acceptable salt thereof; and an anti-emetic/anti-nausea agent or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The NRPA compound and the anti-emetic/anti-nausea agent are present in amounts that render the composition effective modulating cholinergic function or in the treatment of a diorder or condition selected from inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, celiac sprue, pouchitis, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disorders, jet lag, amyotrophic lateral sclerosis (ALS), cognitive dysfunction, hypertension, bulimia, anorexia, obesity, cardiac arrythmias, gastric acid hypersecretion, ulcers, pheochromocytoma, progressive supranuclear palsy, chemical dependencies and addictions (e.g., dependencies on, or addictions to nicotine (and/or tobacco products), alcohol, benzodiazepines, barbiturates, opioids or cocaine), headache, migraine, stroke, traumatic brain injury (TBI), obsessive-compulsive disorder (OCD), psychosis, Huntington's chorea, tardive dyskinesia, hyperkinesia, dyslexia, schizophrenia, multi-infarct dementia, age-related cognitive decline, epilepsy, including petit mal absence epilepsy, senile dementia of the Alzheimer's type (AD), Parkinson's disease (PD), attention deficit hyperactivity disorder (ADHD) and Tourette's Syndrome. The method of using these compositions is also disclosed.
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(2008/06/13)

Chemical Properties

Melting Point: 138.5 °C
Boiling Point: 400.6 °C at 760 mmHg
Flash Point:196.1 °C
Density: 1.247 g/cm³
Solubility:Soluble in DMSO
Vapor Pressure: 1.25E-06mmHg at 25°C
Refractive Index: 1.667
PKA: 9.60±0.20(Predicted)
PSA: 152.87000
LogP: 0.01010

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249296-44-4

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Chemical Properties

Melting Point: 138.5 °C

Boiling Point: 400.6 °C at 760 mmHg

Flash Point:196.1 °C

Density: 1.247 g/cm³

Solubility:Soluble in DMSO

Vapor Pressure: 1.25E-06mmHg at 25°C

Refractive Index: 1.667

PKA: 9.60±0.20(Predicted)

PSA: 152.87000

LogP: 0.01010

Global suppliers and manufacturers of 249296-44-4total 118 suppliers on LookChem

Article Database

249296-44-4

Articles about 249296-44-4Total 14 be found

More Articles about upstream products of 249296-44-4

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Chemical Properties

Melting Point: 138.5 °C

Boiling Point: 400.6 °C at 760 mmHg

Flash Point:196.1 °C

Density: 1.247 g/cm3

Solubility:Soluble in DMSO

Vapor Pressure: 1.25E-06mmHg at 25°C

Refractive Index: 1.667

PKA: 9.60±0.20(Predicted)

PSA: 152.87000

LogP: 0.01010

Global suppliers and manufacturers of 249296-44-4total 118 suppliers on LookChem

Density: 1.247 g/cm³