- SUBSTITUTED (PIPERIDIN-1-YL)ARYL ANALOGUES FOR MODULATING AVILACTIVITY
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In one aspect, the disclosure relates to compounds useful to regulate, limit, or inhibit the expression of AVIL (advillin), methods of making same, pharmaceutical compositions comprising same, and methods of treating disorders associated with AVIL dysregulation using same. In aspects, the disclosed compounds, compositions and methods are useful for treating disorders or diseases in which the regulation, limitation, or inhibition of the expression of AVIL can be clinically useful, such as, for example, the treatment of cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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Paragraph 0369; 0373
(2020/11/12)
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- PYRAZOLOPYRIDAZINE DERIVATIVES, PREPARATION METHOD THEREOF AND COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING THE SAME
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The present invention is a pyrazolopyridazine derivative. A pharmaceutical composition for preventing or treating cancer contains the pyrazolopyridazin derivative compound Hsp90 according to the present invention as an active ingredient, which can be used as Hsp90 a pharmaceutical composition for preventing or treating Hsp90-related diseases such as melanoma, brain tumor, breast cancer, lung cancer and the like. (by machine translation)
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Paragraph 0245-0249
(2020/11/14)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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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. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 30; 31
(2018/03/28)
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- PHARMACEUTICAL COMPOUNDS
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This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated
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Paragraph 0793; 0794; 0795; 0796
(2018/04/26)
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- Discovery, synthesis, biological evaluation and structure-based optimization of novel piperidine derivatives as acetylcholine-binding protein ligands
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The homomeric α7 nicotinic receptor (α7 nAChR) is widely expressed in the human brain that could be activated to suppress neuroinflammation, oxidative stress and neuropathic pain. Consequently, a number of α7 nAChR agonists have entered clinical trials as
- Shen, Jian,Yang, Xi-Cheng,Yu, Ming-Cheng,Xiao, Li,Zhang, Xun-Jie,Sun, Hui-Jiao,Chen, Hao,Pan, Guan-Xin,Yan, Yu-Rong,Wang, Si-Chen,Li, Wei,Zhou, Lu,Xie, Qiong,Yu, Lin-Qian,Wang, Yong-Hui,Shao, Li-Ming
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p. 146 - 155
(2017/01/12)
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- Design and synthesis of novel spiro-piperidinyl pyrazolone derivatives and their potential antiviral activity
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A series of novel spiro-piperidinyl pyrazolones were synthesized starting from the commercially available ethyl nipecotate. The Boc protected ethyl nipecotate was reacted with 5-bromo-2-furaldehyde in the presence of LDA to afford the β -hydroxy ester whi
- Srinivasan, Rajagopalan,Narayana, Badiadka,Sarojini, B. Kunhanna,Bhanuprakash, Veerakyathappa,Raj, Chenna Govindaraju Darshan,Nayak, Prakash S.
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p. 149 - 160
(2016/03/12)
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- COGNITION ENHANCING COMPOUNDS AND COMPOSITIONS, METHODS OF MAKING, AND METHODS OF TREATING
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The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine, receptors and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans. The compositions comprising a muscarinic agonist or a pharma.ceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.
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Page/Page column 145-146
(2012/03/27)
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- COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING
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Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
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Page/Page column 124
(2011/08/03)
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- COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING
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Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.
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Page/Page column 117-118
(2010/09/18)
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- Synthesis of 3-(3-piperidyl)-isoquinoline and 3-(4-piperidyl)-isoquinoline
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3-(3-Piperidyl)isoquinoline and 3-(4-piperidyl)isoquinoline have been synthesized from o-tolylaldehyde aldimines and the methylmethoxycarboxamides (Weinreb amides) of N-Boc-substituted nipecotic and isonipecotic acids.
- Kovalskiy,Perevalov
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experimental part
p. 957 - 964
(2010/03/26)
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- Convenient synthesis of 1,1′-H-spiro[indoline-3,3′-piperidine]
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The spirocyclic indoline ring system represents an important scaffold for the discovery of novel therapeutics. Herein, we describe the synthesis of 1,1′-H-spiro[indoline-3,3′-piperidine] using an intramolecular palladium-catalyzed α-arylation reaction.
- Pfefferkorn, Jeffrey A.,Choi, Chulho
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p. 4372 - 4373
(2008/12/21)
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- PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
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Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
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Page/Page column 126
(2008/06/13)
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- Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors
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Structure-based methods were used to design β-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based
- Lombart, Henry-Georges,Feyfant, Eric,Joseph-McCarthy, Diane,Huang, Adrian,Lovering, Frank,Sun, LinHong,Zhu, Yi,Zeng, Congmei,Zhang, Yuhua,Levin, Jeremy
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p. 4333 - 4337
(2008/02/11)
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- Synthesis of novel 5-piperidyl-substituted 7-hydroxy-3H-1,2,3-triazolo [4,5-d]pyrimidines
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A series of 8-azapurin-6-ones having a piperidine substituent at position 5 has been synthesized from pipecolinate esters, benzylazides, and cyanoacetamide. 2006 Springer Science+Business Media, Inc.
- Kuleshov,Borovkov,Rodin,Perevalov
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p. 246 - 260
(2007/10/03)
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- HETEROCYCLIC SPIRO COMPOUND
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The compound represented by formula (I) (wherein D and G are cyclic group which may have a substituent(s) or alkyl which may have a substituent(s), W and Y are a bond or a spacer of which main chain has an atom number of 1-4, ringA and ringB are heterocyc
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Page/Page column 33
(2008/06/13)
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- ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS
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Compounds of the formula:useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
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Page/Page column 24; 38
(2010/02/14)
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- Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha
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The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3
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Page/Page column 49
(2010/11/30)
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- Gem-substituted αvβ3 antagonists
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The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αVβ3and/or the αVβ5integrin.
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- Pyridine derivatives
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Pyridine compounds of general formula: wherein —R1represents in which R11is hydrogen, C1-6alkyl, halogen, hydroxy, C1-12alkoxy, nitro, amino, C1-6alkylsulfonylamino, C1-6alkoxycarbonyl, C1-6alkylamino, di(C1-6alkyl)amino, C1-6alkanoylamino, phenyl C1-6alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2represents hydrogen or halogen; R3represents hydrogen, —CR31R32R33, or —NR34R35; R4is hydrogen, carbamoyl, CN, carboxyl, etc.; R5is amino, C1-6alkylamino, di C1-6alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
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- Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors
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Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
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- Method for preparing alpha-sulfonyl hydroxamic acid derivatives
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Compounds of the formula: that can be important as matrix metalloproteinase (MMP) and TNF-alpha converting enzyme (TACE) inhibitors, phosphodiesterase inhibitors, renin inhibitors, antithrombotics, and 5-lipoxygenase inhibitors are prepared by novel methods of the present invention.
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- Thiourea-based gemfibrozil analogues as HDL-elevating agents.
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A series of gemfibrozil analogues with a thiourea moiety embedded in the side chain was prepared and evaluated as HDL-elevating agents. Derivatives 8b, 9b, 9c, and 9d were found to be approximately as effective as gemfibrozil (1) for HDL cholesterol eleva
- Coppola, Gary M,Damon, Robert E,Eskesen, J Bruce,France, Dennis S,Paterniti Jr., James R
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p. 2439 - 2442
(2007/10/03)
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- Synthesis of potent and highly selective inhibitors of human tryptase
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The serine protease tryptase has been implicated in allergic and inflammatory diseases and associated with asthma. The synthesis and SAR of a series of N1-activated-4-carboxy azetidinones are described, resulting in identification of BMS-363131 (2) as a potent inhibitor of human tryptase (IC503000-fold) for tryptase versus related serine proteases including trypsin.
- Slusarchyk, William A.,Bolton, Scott A.,Hartl, Karen S.,Huang, Ming-Hsing,Jacobs, Glenn,Meng, Wei,Ogletree, Martin L.,Pi, Zulan,Schumacher, William A.,Seiler, Steven M.,Sutton, James C.,Treuner, Uwe,Zahler, Robert,Zhao, Guohua,Bisacchi, Gregory S.
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p. 3235 - 3238
(2007/10/03)
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- Beta lactam compounds and their use as inhibitors of tryptase
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Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.
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Page column 210
(2010/11/29)
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- Compound with growth hormone releasing properties
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The present invention describes a new compound, 2-Amino-N-[(1R)-2-[(3R)-3-benzyl-3-(N,N′,N′-trimethylhydrazinocarbonyl)piperidin-1-y]-1-(1H-indol-3-ylmethyl)-2-oxoethyl]-2-methylpropionamide, having the formula: and pharmaceutically acceptable salts thereof, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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- Towards a new synthetic entry into the Iboga-alkaloid family
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A novel retrosynthetic concept is presented that, in principle, allows access to many hitherto not accessible representatives of the Iboga-alkaloid family. The flexibility required by this approach is provided through a highly convergent assembly of the target, which allows for a control over the substitution pattern of the indole sub-system, as well as over the relative configuration of the aliphatic core of these alkaloids. The key step for the construction of the latter consists in an intramolecular nitrone-olehn 1,3-dipolar cycloaddition reaction of 26 to yield the crucial tricyclic isoxazolidine derivative 28.
- Frauenfelder, Christine,Borschberg, Hans-Juerg
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p. 1753 - 1765
(2007/10/03)
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- Thiazole-derived potent, highly bioavailable short duration growth hormone secretagogues
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Replacement of the phenyl in 3 with a 2-pyridyl or 4-thiazolyl group resulted in increased potency in the rat pituitary cell GH release assay and in beagles.
- Yang, Lihu,Morriello, Greg,Leung, Kwan,Jacks, Tom,Cheng, Kang,Schleim, Klaus D.,Smith, Roy,Patchett, Arthur A.
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p. 1761 - 1766
(2007/10/03)
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- Synthesis of a Novel Heterospirocyclic 3-(N-Methyl-N-phenylamino)-2H-azirine and its Use as an Amino Acid Equivalent in the Preparation of a Model Tripeptide
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The synthesis of a novel heterospirocyclic 3-amino-2H-azirine based on the reaction between amide enolates and diphenylphosphorochloridate is described.This compound has been shown to be a useful amino acid equivalent and the synthesis of a model tripepti
- Villalgordo, Jose M.,Heimgartner, Heinz
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p. 7215 - 7222
(2007/10/02)
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