Tag: M.W:100-200

27578-60-5, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 27578-60-5, Name is N-(2-Aminoethyl)piperidine, molecular formula is C7H16N2. In a Article, authors is Papeo, Gianluca£¬once mentioned of 27578-60-5

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy

The nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) has a well-established role in the signaling and repair of DNA and is a prominent target in oncology, as testified by the number of candidates in clinical testing that unselectively target both PARP-1 and its closest isoform PARP-2. The goal of our program was to find a PARP-1 selective inhibitor that would potentially mitigate toxicities arising from cross-inhibition of PARP-2. Thus, an HTS campaign on the proprietary Nerviano Medical Sciences (NMS) chemical collection, followed by SAR optimization, allowed us to discover 2-[1-(4,4-difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118, 20by). NMS-P118 proved to be a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles and high efficacy in vivo both as a single agent and in combination with Temozolomide in MDA-MB-436 and Capan-1 xenograft models, respectively. Cocrystal structures of 20by with both PARP-1 and PARP-2 catalytic domain proteins allowed rationalization of the observed selectivity.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H4262N – PubChem

 

106-52-5, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 106-52-5, molcular formula is C6H13NO, introducing its new discovery.

ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette”s syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

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Piperidine – Wikipedia,
Piperidine | C5H2360N – PubChem

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, 50541-93-0, such as the rate of change in the concentration of reactants or products with time.In a article, authors is Mitsuya, mentioned the application of 50541-93-0, Name is 4-Amino-1-benzylpiperidine, molecular formula is C12H18N2

A potent, long-acting, orally active (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: A novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors

A novel series of (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamides was designed and synthesized based on the structure and biological profiles of an active metabolite 2 of our prototype muscarinic M3 receptor selective antagonist 1, to develop a potent, long-acting, orally active M3 antagonist for the treatment of urinary tract disorders, irritable bowel syndrome, and respiratory disorders. Investigation of (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamides containing a phenyl or heterocyclic ring as the piperidinyl side chain in place of the 4-methyl-3-pentenyl moiety of 15a revealed that this acid moiety was a versatile template for improving the selectivity for M3 over M2 receptors in comparison with the corresponding cyclopentylphenylacetic acid group. However, since the in vitro metabolic stability of these analogues was insufficient compared with that of 2, further derivatization was performed by introducing an appropriate hydrophilic group into the phenyl or 2-pyridyl ring. Thus, the 1-(6-aminopyridin-2-ylmethyl)piperidine analogue 15y exhibiting 190-fold selectivity for M3 receptors (Ki = 2.8 nM) over M2 receptors (Ki = 530 nM) in a human binding assay and good in vitro metabolic stability in dog and human hepatic microsomes was identified. This compound has excellent oral activity at 4 h after oral dosing (1 mg/kg), inhibiting methacholine-induced bronchoconstriction in dogs, and may be useful in clinical situations in which M3 over M2 selectivity is desirable.

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Piperidine – Wikipedia,
Piperidine | C5H12032N – PubChem

 

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 177-11-7, Name is 1,4-Dioxa-8-azaspiro[4.5]decane. In a document type is Article, introducing its new discovery., 177-11-7

Synthesis of carbamates and ureas using Zr(IV)-catalyzed exchange processes

Equation presented Zirconium(IV)-catalyzed exchange processes have been developed to prepare both carbamates and ureas from dialkyl arbonates and carbamates employing 2-hydroxypyridine (HYP) and 4-methyl-2-hydroxyquinoline (MeHYQ) as catalytic additives, respectively A microwave acceleration effect was observed in Zr(IV)-catalyzed carbamate-urea exchange.

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Piperidine – Wikipedia,
Piperidine | C5H7591N – PubChem

 

Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 50541-93-0, molcular formula is C12H18N2, introducing its new discovery. 50541-93-0

Use of substituted chromans, some of which are known, as medicaments, new active compounds and processes for their preparation

The present invention relates to the use of substituted chromans of the general formula (I) STR1 in which the substituents have the meaning indicated in the description, for the production of medicaments, in particular as HIV protease-inhibiting agents, new active compounds and processes for their preparation.

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Piperidine – Wikipedia,
Piperidine | C5H12222N – PubChem

 

Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2008-75-5, molcular formula is C7H15Cl2N, introducing its new discovery. 2008-75-5

Quinazoline derivatives

The invention concerns quinazoline derivatives of the formula I STR1 wherein n is 1, 2 or 3 and each R2 is independently halogeno, trifluoromethyl or (1-4C)alkyl; R3 is (1-4C)alkoxy; and R1 is di-?(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-?(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R1 substituents comprising a CH2 (methylene) group which is not attached to a N or O atom optionally bears on said CH2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.

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Piperidine – Wikipedia,
Piperidine | C5H11149N – PubChem

 

1484-84-0, Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 1484-84-0, Name is 2-Piperidineethanol

A ring-closing yne-carbonyl metathesis of ynamides

An acid-catalyzed ring-closing ynamide-carbonyl metathesis is described here. This hetero RCM methodology is applicable to the construction of carbocycles as well as heterocycles such as chromenes, quinolizidines, indolizidines, and pyrrolizidines.

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Piperidine – Wikipedia,
Piperidine | C5H5671N – PubChem

 

In homogeneous catalysis, the catalyst is in the same phase as the reactant. 24666-56-6. The number of collisions between reactants and catalyst is at a maximum.In a patent, 24666-56-6, name is 3-Aminopiperidine-2,6-dione hydrochloride, introducing its new discovery.

SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders as well as other disorders.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.24666-56-6, you can also check out more blogs about24666-56-6

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Piperidine – Wikipedia,
Piperidine | C5H9542N – PubChem

 

39546-32-2, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 39546-32-2, C6H12N2O. A document type is Article, introducing its new discovery.

Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer’s disease

Acetylcholinesterase (AChE) is the key enzyme targeted in Alzheimer’s disease (AD) therapy, nevertheless butyrylcholinesterase (BuChE) has been drawing attention due to its role in the disease progression. Thus, we aimed to synthesize novel cholinesterases inhibitors considering structural differences in their peripheral site, exploiting a moiety replacement approach based on the potent and selective hAChE drug donepezil. Hence, two small series of N-benzylpiperidine based compounds have successfully been synthesized as novel potent and selective hBuChE inhibitors. The most promising compounds (9 and 11) were not cytotoxic and their kinetic study accounted for dual binding site mode of interaction, which is in agreement with further docking and molecular dynamics studies. Therefore, this study demonstrates how our strategy enabled the discovery of novel promising and privileged structures. Remarkably, compound 11 proved to be one of the most potent (0.17 nM) and selective (>58,000-fold) hBuChE inhibitor ever reported.

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Piperidine – Wikipedia,
Piperidine | C5H3597N – PubChem

 

Chemistry is traditionally divided into organic and inorganic chemistry. 41838-46-4. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 41838-46-4

DIHYDROBENZO[B][1]BENZOTHIEPIN COMPOUNDS USEFUL IN THERAPY

The present invention relates to the use of a compound of formula (I), to decrease or inhibit, in vitro or ex vivo, the Patched receptor drug efflux activity, in particular the chemotherapeutic drug efflux activity and chemotherapy resistance. The present disclosure further relates to uses of such compounds, in particular to prepare a pharmaceutical composition to allow or improve the efficiency of a therapy of cancer in a subject in need thereof. The compound of the invention can indeed be advantageously used, in combination with at least one chemotherapeutic drug, for treating cancer, for preventing cancer metastasis and/or for preventing cancer recurrence in a subject.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 41838-46-4 is helpful to your research. 41838-46-4

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H1722N – PubChem