- NON-FUSED TRICYCLIC COMPOUNDS
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Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
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Paragraph 00561
(2018/11/26)
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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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Paragraph 0120
(2016/03/19)
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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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Page/Page column 58
(2016/05/19)
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- Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists
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A series of alkylpyrimidine-4,6-diol derivatives were designed and synthesized as novel GRP84 agonists based on a high-throughput screening (HTS) hit 1. 6-Nonylpyridine-2,4-diol was identified as the most potent agonist of GPR84 reported so far, with an EC50 of 0.189 nM. These novel GPR84 agonists will provide valuable tools for the study of the physiological functions of GPR84.
- Liu, Yang,Zhang, Qing,Chen, Lin-Hai,Yang, Hui,Lu, Wei,Xie, Xin,Nan, Fa-Jun
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supporting information
p. 579 - 583
(2016/07/06)
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- MUSCARINIC AGONISTS
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Compounds of formula (I) and methods are provided for the treatment of disease or conditions in which modification of cholinergic, especially muscarinic receptor activity, has a beneficial effect.
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Paragraph 0195
(2014/10/04)
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- DNA-dependent protein kinase (DNA-PK) inhibitors: Structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain
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Introduction of an O-alkoxyphenyl substituent at the 8-position of the 2-morpholino-4H-chromen-4-one pharmacophore enabled regions of the ATP-binding site of DNA-dependent protein kinase (DNA-PK) to be probed further. Structure-activity relationships have been elucidated for inhibition of DNA-PK and PI3K (p110α), with N-(2-(cyclopropylmethoxy)-4-(2-morpholino-4-oxo-4H- chromen-8-yl)phenyl)-2-morpholinoacetamide 11a being identified as a potent and selective DNA-PK inhibitor (IC50 = 8 nM).
- Clapham, Kate M.,Bardos, Julia,Finlay, M. Raymond V.,Golding, Bernard T.,Griffen, Edward J.,Griffin, Roger J.,Hardcastle, Ian R.,Menear, Keith A.,Ting, Attilla,Turner, Paul,Young, Gail L.,Cano, Céline
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body text
p. 966 - 970
(2011/03/20)
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- COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Disclosed herein are cannabinoid receptor ligands of formula (1) wherein Ring A and R1 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also described
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Page/Page column 25
(2010/10/19)
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- NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
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Page/Page column 52
(2010/04/23)
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- Peptide deformylase inhibitors with retro-amide scaffold: Synthesis and structure-activity relationships
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Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies. Reported herein are the synthesis
- Lee, Seung Kyu,Choi, Kwang Hyun,Lee, Sang Jae,Suh, Se Won,Kim, B. Moon,Lee, Bong Jin
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body text
p. 4317 - 4319
(2010/10/03)
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- PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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Page/Page column 45-46
(2009/10/30)
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- Aromatic compounds and pharmaceutical compositions containing them
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The invention relates to compounds of formula I and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof and processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
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- Kinetics and mechanism of the aminolysis of cycloalkylmethyl arenesulfonates
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Nucleophilic substitution reactions of cycloalkylmethyl arenesulfonates (CmH2n-1 CH2OSO2C6H4Z) with anilines (XC6H4NH2) in methanol at 65.0 °C were studied. The reactivity order (n=4>6>7>5) reflects largely the order of steric effect of the ring size (SEs term) except for n=5, which exhibits the least reactivity. This reversal of the order for n=5 is considered to result from large rate retardation due to polar effect of the ρ*σ* term. Application of the Taft equation to the rate data for n=5 and 6 gives ρ=17·4 and 5=2·3 with correlation coefficient of 0·90. The σ* values for n=4 and 7 are estimated to be - 0·23 and - 0·11, respectively. The positive ρxz values of ca 0·3 are consistent with previous results for the reactions at primary reaction centers.
- Oh, Hyuck Keun,Song, Se Jeong,Jo, Dong-Soo,Lee, Ikchoon
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- General Synthesis of Methyl- and Dimethyl-cyclobutanes from Simple 1,3-Diols by Phase Transfer Catalysis
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A general method is described for the preparation of methyl- and dimethyl-cyclobutanes from simple 1,3-diols.The key steps of the procedure are a phase transfer catalysed ring closure and the transformation of a carboxyl group to a methyl group.Phase transfer catalysis provides good yields in the synthesis of the cyclobutane skeleton.
- Toeroek, Bela,Molnar, Arpad
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p. 801 - 804
(2007/10/02)
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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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- LONG-ACTING CONTRACEPTIVE AGENTS: CYCLOPROPYL AND CYCLOBUTYL ESTERS OF NORETHISTERONE
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Several esters of norethisterone (17α-ethynyl-17β-hydroxyestr-4-en-3-one) with carboxylic acids containing a cyclopropyl or cyclobutyl ring have been synthesized and the stereochemistries of the side-chains determined.
- Shafiee, A.,Vossoghi, M.,Savabi, F.,Vlahov, R.,Tarpanov, V.,et al.
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p. 291 - 308
(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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- The Kinetics and Mechanism of Ring Opening of Radicals containing the Cyclobutylcarbinyl System
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The kinetic parameters of β-fission of radicals containing the cyclobutylcarbinyl system have been determined by analysis of the mixtures obtained when suitable chloro-compounds are treated with tributylstannane.Under these conditions ring opening is irreversible and in the rigid bicyclic system (4) is under stereoelectronic control.For ring opening of cyclobutylcarbinyl radical (8) kf = 4.3 x 103 s-1 at 60 deg C, and the best values of the activation parameters appear to be ΔH(excit.) = 12.2 kcal mol-1 and ΔS(excit.) = -7.4 cal mol-1 K-1.Monocyclic systems undergo preferential fission of the more substituted βγ-bond.Methyl substituents at the α-, β-, or δ-positions have little effect but γ-substitution strongly enhances the rate of ring opening.The transition state is reactant-like and has a similar disposition of centres to that (1) for homolytic addition.
- Beckwith, Athelstan L. J.,Moad, Graeme
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p. 1083 - 1092
(2007/10/02)
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