400828-91-3Relevant articles and documents
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models
Kamakolanu, Uma Gayathri,Meyer, Michael E.,Yasuda, Dennis,Polgar, Willma E.,Marti, Matteo,Mercatelli, Daniela,Pisanò, Clarissa Anna,Brugnoli, Alberto,Morari, Michele,Zaveri, Nurulain T.
, p. 2688 - 2704 (2020/03/31)
A novel series of C(3)-substituted piperdinylindoles were developed as nociceptin opioid receptor (NOP) partial agonists to explore a pharmacological hypothesis that NOP partial agonists would afford a dual pharmacological action of attenuating Parkinson'
ANTI-INFECTIVE HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Page/Page column 18; 21; 22, (2019/05/22)
The present invention relates to heterocyclic compounds of Formula F-I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.
PIPERDINYL NOCICEPTIN RECEPTOR COMPOUNDS
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Paragraph 0147-0149, (2018/06/15)
The present invention provides novel piperidinyl-containing nociceptin receptor ligand compounds and pharmaceutical compositions useful in the treatment of neurological diseases and conditions where such ligands mediate the negative effects of the condition. Such neurological diseases and conditions include acute and chronic pain, substance abuse/dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, renal disorders, cardiovascular disorders and Parkinson's disease.
PIPERIDINYL NOCICEPTIN RECEPTOR COMPOUNDS
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Page/Page column 101; 102, (2017/12/28)
The present invention provides novel piperidinyl-containing nociceptin receptor ligand compounds and pharmaceutical compositions useful in the treatment of neurological diseases and conditions where such ligands mediate the negative effects of the condition. Such neurological diseases and conditions include acute and chronic pain, substance abuse/dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, renal disorders, cardiovascular disorders and Parkinson' s disease.
MULTIVALENT RAS BINDING COMPOUNDS
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Paragraph 00905, (2017/07/23)
Described herein are compounds that modulate Ras signaling, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with altered Ras signaling. Further described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds and methods of using such compounds in the treatment of cell proliferative disorders, including cancer.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: Part 2. Pyridazine-based analogs
Yang, Shyh-Ming,Tang, Yuting,Rano, Thomas,Lu, Huajun,Kuo, Gee-Hong,Gaul, Michael D.,Li, Yaxin,Ho, George,Lang, Wensheng,Conway, James G.,Liang, Yin,Lenhard, James M.,Demarest, Keith T.,Murray, William V.
supporting information, p. 1437 - 1441 (2014/03/21)
Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1) inhibitors are described. In a chronic study of selected analog (3e) in Zucker fa/fa (ZF) rat, dose-dependent decrease of body weight gain and plasma fatty acid desaturation index (DI) in both C16 and C18 are also demonstrated. The results indicate that the plasma fatty acid DI may serve as an indicator for direct target engagement and biomarker for SCD1 inhibition.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs
Yang, Shyh-Ming,Tang, Yuting,Zhang, Rui,Lu, Huajun,Kuo, Gee-Hong,Gaul, Michael D.,Li, Yaxin,Ho, George,Conway, James G.,Liang, Yin,Lenhard, James M.,Demarest, Keith T.,Murray, William V.
supporting information, p. 6773 - 6776 (2014/01/06)
A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure-activity relationships focused on bicyclic heteroarenes and aminothiazole-urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated.
Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5- yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine
Annedi, Subhash C.,Maddaford, Shawn P.,Ramnauth, Jailall,Renton, Paul,Rybak, Taras,Silverman, Sarah,Rakhit, Suman,Mladenova, Gabriela,Dove, Peter,Andrews, John S.,Zhang, Dongqin,Porreca, Frank
, p. 94 - 107,14 (2020/07/31)
We recently reported a series of 1,6-disubstituted indoline-based thiophene amidine compounds (5) as selective neuronal nitric oxide synthase (nNOS) inhibitors to mitigate the cardiovascular liabilities associated with hERG K+ channel inhibition (IC50 = 4.7 μM) with previously reported tetrahydroquinoline-based selective nNOS inhibitors (4). The extended structure-activity relationship studies within the indoline core led to the identification of 43 as a selection candidate for further evaluations. The in vivo activity in two different pain (spinal nerve ligation and migraine pain) models, the excellent physicochemical and pharmacokinetic properties, oral bioavailability (Fpo = 91%), and the in vitro safety profile disclosed in this report make 43 an ideal candidate for further evaluation in clinical applications related to migraine pain.
1-PIPERIDINYL-6-PIPERIDINYLSULFONYLINDOLES AS 5-HT (2B) RECEPTOR ANTAGONISTS
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Page/Page column 14, (2009/03/07)
The present invention relates to novel indole derivatives which bind to the 5-HT2B receptor and are capable of interfering with the effects of 5-hydroxytryptamine (5-HT) at the 5-HT2B receptor; to processes for their preparation; to pharmaceutical compositions containing them; and to the use of such compounds in therapy.
NOVEL COMPOUNDS
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Page/Page column 13-14, (2009/03/07)
The present invention relates to novel indoline derivatives which bind to the 5-HT2B receptor and are capable of interfering with the effects of 5-hydroxytryptamine (5-HT) at the 5-HT2B receptor; to processes for their preparation; to pharmaceutical compositions containing them; and to the use of such compounds in therapy.