- Rate constants and Arrhenius functions for ring opening of a cyclobutylcarbinyl radical clock and for hydrogen atom transfer from the Et 3B-MeOH complex
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(Chemical Equation Presented) Kinetics of ring opening of the 1-cyclobutyldodecyl radical (1) were studied, and an Arrhenius function over the temperature range -20 to 47°C was determined. The radical clock reaction has kinetics described by log k = 13.2-13.5/2.313RT (in kcal/mol), and k = 1.5 × 103 s-1 at 20°C. Previous kinetic studies of hydrogen atom transfer trapping of radical 1 by the triethylborane-methanol complex at variable temperatures (J. Org. Chem. 2007, 72, 5098) were analyzed with the newly obtained kinetic data.
- Jin, Jing,Newcomb, Martin
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Read Online
- TRISUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINE COMPOUNDS AS CDK7 INHIBITORS
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Compounds having activity as cancer agents are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salts, stereoisomers, tautomers, thereof, wherein R1, R2, R3 and L are as defined herein. This disclosure provides methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds, and methods for treating a CDK7-dependent disease (e.g., cancer).
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Page/Page column 69
(2020/09/27)
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- Formal reductive addition of acetonitrile to aldehydes and ketones
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An efficient and highly productive rhodium-catalyzed method for the synthesis of nitriles employing aldehydes or ketones, methyl cyanoacetate, water and carbon monoxide as starting materials has been developed. Simple rhodium chloride without any ligands can be used. The fine tuning of the substrate can lead to the activity higher than 5000 TON.
- Muratov, Karim,Kuchuk, Ekaterina,Vellalath, Sreekumar,Afanasyev, Oleg I.,Moskovets, Alexei P.,Denisov, Gleb,Chusov, Denis
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supporting information
p. 7693 - 7701
(2018/11/02)
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- PYRAZOLE PYRIMIDINE DERIVATIVE AND USES THEREOF
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The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or lnterleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.
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Page/Page column 62
(2017/02/28)
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- Piperazine derivatives and their use as therapeutic agents
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Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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- THIAZOLES AS MODULATORS OF RORyt
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The present invention comprises compounds of Formula I. Formula I wherein: R1, R2, R3, R4, R5, R7, R8, and (A) are defined in the specification. The invention also comprises a co
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- SYNTHESIS OF TELAPREVIR AND BOCEPREVIR, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR SOLVATES AS WELL AS INTERMEDIATE PRODUCTS THEREOF INCLUDING ?-AMINO ACIDS PREPARED VIA MUKAIYAMA ALDOL ADDITION
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The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.
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Page/Page column 51
(2014/01/09)
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- PROCESS AND INTERMEDIATES FOR THE PREPARATION OF 3-AMINO-4-CYCLOBUTYL-2-HYDROXYBUTANAMIDE AND SALTS THEREOF
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The present invention relates to synthetic processes useful in the preparation of a compound of Formula (I), and salts thereof. Compounds of Formula (I) and salts thereof have application in the preparation of inhibitors of the hepatitis C virus, such as (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6, 6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
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- CARBOXAMIDE 4-[(4-PYRIDYL)AMINO]PYRIMIDINES USEFUL AS HCV INHIBITORS
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The present invention relates to the use of carboxamide 4-[(4-pyridyl)amino]- pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections.
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Page/Page column 43
(2008/06/13)
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- 4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties
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A systematic examination of the central aromatic portion of the lead (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(1′H-spiro[indene-1,4′-piperidin]-1′-yl)butanamide (9) led to the discovery of a novel class of CCR2 receptor antagonists, which carry small alicyclic groups such as cyclopropyl, cylobutyl, or cyclopropylmethyl attached at C2 of the carbon backbone. The most potent compound discovered, namely (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-cyclopropyl-4-[(1R,3′R)-3′-methyl-1′H-spiro[indene-1,4′-piperidin]-1′-yl]butanamide (29), showed very high binding affinity (IC50 = 4 nM, human monocyte) and excellent selectivity toward other related chemokine receptors. The excellent pharmacokinetic profile of this new lead compound allows for extensive in vivo evaluation.
- Butora, Gabor,Morriello, Gregori J.,Kothandaraman, Shankaran,Guiadeen, Deodialsingh,Pasternak, Alexander,Parsons, William H.,MacCoss, Malcolm,Vicario, Pasquale P.,Cascieri, Margaret A.,Yang, Lihu
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p. 4715 - 4722
(2007/10/03)
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- CARBOXAMIDE INHIBITORS OF TGFB
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Certain appropriately substituted forms of pyrimidine having a pyridylamine group at C- 4 of the pyrimidine and an amide group on the pyridine ring are useful in the treatment of conditions associated with excessive TGFB activity.
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Page/Page column 27; 43-44
(2010/11/24)
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- Discovery of new antitubercular oxazolyl thiosemicarbazones
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Twenty 4-(5-cyclobutyloxazol-2-yl)thiosemicarbazones were synthesized and evaluated for preliminary in vitro and in vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Among them, (4-br
- Sriram, Dharmarajan,Yogeeswari, Perumal,Thirumurugan, Rathinasababathy,Pavana, Roheet Kumar
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p. 3448 - 3450
(2007/10/03)
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- PYRAZOLINES AS PAR-1 ANTAGONISTS FOR TREATMENT OF CARDIOVASCULAR DISEASES
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The invention relates to pyrazolines of formula (I), where E = methylene, NH, O or S and R2 = a group of formula (II), methods for the production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular, cardiovascular diseases, such as thromboembolitic diseases.
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Page/Page column 51
(2010/02/10)
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- INHIBITORS OF TFGβ
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Certain appropriately substituted forms of pyrimidine and triazine are useful in the treatment to conditions associated with enhanced TGFβ activity.
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Page/Page column 33; 34
(2010/02/06)
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- Gamma amino butyric and acid analogs
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The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation.
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- Pyrazinone thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: for example:
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- Synthesis and Liquid Crystal Properties of Dimethylene Linked Compounds Incorporating the Cyclobutane or Spiroheptane Rings
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The preparation of sixteen dimethylene linked compounds is described heptane ring>, and a comparison is made between the transition temperatures of these compounds and those of the corresponding esters.This comparison once again highlights the fact that the cyclobutane ring should be regarded, in terms of its ability to promote nematic thermal stability, as a "chain stiffener rather than as a ring system.A comparison is also made of the nematic thermal stabilities of the trans-cyclobutane and the spiroheptane systems and of the trans-cyclohexane and the spiroundecane systems.
- Chan, L. K. M.,Gemmell, P. A.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 229 - 246
(2007/10/02)
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- Cyclobutyl substituted derivatives of prostaglandin analogs
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Novel C15 cyclobutyl analogs or derivatives of prostaglandins of the E-, A- and F-classes are useful modifiers of smooth muscle activity. The compounds have valuable pharmacological properties such as platelet antiaggregating agents, gastric antisecretory agents and brochodilating agents.
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