198821-79-3Relevant articles and documents
Optimization of a hydrogenation process using real-time mid-IR, heat flow and gas uptake measurements
Littler, Benjamin J.,Looker, Adam R.,Blythe, Todd A.
, p. 1512 - 1517 (2010)
This paper describes using real-time mid-IR, heat flow, and gas uptake data to optimize the hydrogenation of a nitroaromatic to an aniline that had been difficult to control during a previous campaign in the pilot plant. A bimetallic Pt/V catalyst was identified that eliminated the buildup of reaction intermediates and consequently resulted in an inherently more controllable process. The real-time analytics were then used to rapidly optimize the reaction conditions and develop strategies for controlling the reaction rate in the plant should an unexpected deviation occur.
Discovery, Structure-Activity Relationships, and in Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain
Hartz, Richard A,Ahuja, Vijay T.,Nara, Susheel J.,Kumar, C.M. Vijaya,Brown, Jeffrey M.,Bristow, Linda J.,Rajamani, Ramkumar,Muckelbauer, Jodi K.,Camac, Daniel,Kiefer, Susan E.,Hunihan, Lisa,Gulianello, Michael,Lewis, Martin,Easton, Amy,Lippy, Jonathan S.,Surti, Neha,Pattipati, Sreenivasulu N.,Dokania, Manoj,Elavazhagan, Saravanan,Dandapani, Kumaran,Hamman, Brian D.,Allen, Jason,Kostich, Walter,Bronson, Joanne J.,Macor, John E.,Dzierba, Carolyn D.
, p. 11090 - 11128 (2021/08/03)
Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to the d
NEW COMPOUNDS AND THEIR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR PREVENTION OF DISEASES INVOLVING THE RETINAL PIGMENT EPITHELIUM
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, (2022/01/05)
The present invention relates to new compounds and to their use as therapeutically active substances in the treatment and/or prevention of diseases involving the retinal pigment epithelium, and in particular in the treatment and/or prevention of diseases
N-(4-(OXAZOL-5-YL)PHENYL)CHROMANE-3-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS STIMULATORS OF THE PRODUCTION OF RETINAL PRECURSOR CELLS FOR THE TREATMENT OF NEURORETINAL DISEASES
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, (2020/07/15)
New compounds and to a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, comprising administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enant
ARYL AMIDE KINASE INHIBITORS
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, (2015/02/02)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
QUINOLINE-BASED KINASE INHIBITORS
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, (2015/11/02)
The present disclosure is generally directed to compounds of formula (I) which can inhibit AAKI (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAKI.
SUBSTITUTED HETEROCYCLIC DERIVATIVES
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, (2014/06/11)
The present invention relates to compounds of general formula (I-1) or (I-2) wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; R1' is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; with the proviso that both R1 and R1' may be simultaneously hydrogen, but only one of R1 and R1' is lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; Het is a 5-or 6 membered heteroaryl group, wherein the heteroatom is selected from N, O or S; X is -CRR'-, -CRR'-NR'-, -C(O)-, -CH2-S-, -CH2-S(O)2-, CH2-O- or -CH2-CRR'-; R/R' are independently from each other hydrogen, lower alkyl, hydroxy or phenyl, or R and R' may form together with the carbon atom to which they are attached a cyclopropyl ring; R2 is lower alkyl, -C(O)O-lower alkyl, C3-6-cycloalkyl optionally substituted by lower alkyl or =O, bridged cyclohexyl or C3-6-cycloalkenyl, or is a 5-membered heteroaryl group, wherein the heteroatom is selected from N, O or S and which is optionally substituted by one or more lower alkyl, or is pyridinyl, optionally substituted by halogen or lower alkoxy; or is phenyl, optionally substituted by one or more R2', selected from halogen, cyano, S(O)2-lower alkyl, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or amino, or is benzo[1,3]dioxolyl, naphthyl, indolyl, benzo-isoxazolyl, 2,3-dihydro-1H-indenyl, optionally substituted by lower alkoxy or by an oxo group, or is 3,4-dihydro-2H- [1,4]oxazinyl, optionally substituted by an oxo group, or is a five or six membered heterocycloalkyl group; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
Development and manufacture of the inosine monophosphate dehydrogenase inhibitor merimepodib, VX-497
Looker, Adam R.,Littler, Benjamin J.,Blythe, Todd A.,Snoonian, John R.,Ansell, Graham K.,Jones, Andrew D.,Nyce, Phil,Chen, Minzhang,Neubert, Bobbianna J.
, p. 666 - 673 (2013/01/03)
A process for the manufacture of merimepodib (VX-497), an inosine monophosphate dehydrogenase (IMPDH) inhibitor, has been developed and efficiently scaled to produce clinical supply. The process comprises five steps, incorporating simple and robust chemis
A new efficient synthesis of 5-aryloxazoles from arylidene diacetates and application to the preparation of BMS-337197, a novel IMPDH inhibitor
Chen, Bang-Chi,Bednarz, Mark S.,Zhang, Huiping,Zhao, Rulin,Murali,Balu Balasubramanian, Dhar,Barrish, Joel C.
, p. 167 - 173 (2007/10/03)
A new method for the synthesis of 5-aryloxazoles is described. Treatment of arylidene diacetates with one equivalent of TosMIC reagent in the presence of excess of potassium carbonate in methanol afforded 5-aryloxazoles in "one-pot" in 90-94%. Heteroaryli
PROCESSES FOR PREPARING BIARYL UREAS AND ANALOGS THEREOF
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Page/Page column 53; 60-61, (2008/06/13)
The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.