- IRAK DEGRADERS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same.
- -
-
Paragraph 00101; 00102-00103
(2021/08/13)
-
- 3-(dimethylaminomethyl) cyclohex-4-alcohol derivative as well as preparation method and pharmaceutical application thereof
-
The invention belongs to the field of pharmacy, and relates to a 3-(dimethylaminomethyl) cyclohex-4-alcohol derivative with a general formula (I) or a salt thereof and a preparation method, and relates to an application of the compound in treatment of opioid receptor mediated diseases. The present invention provides a pharmaceutically acceptable solvate or hydrate of a compound of formula (I), and also provides a pharmaceutical composition comprising: a compound of formula (I) or a pharmaceutically acceptable salt, solvate or hydrate thereof; and a pharmaceutically acceptable carrier. The medicine prepared from the compound can be used for treating or improving diseases related to an opioid receptor; wherein the diseases can be selected from but not limited to pain, gastrointestinal diseases and depression.
- -
-
Paragraph 0324-0327
(2021/05/08)
-
- LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY ELEMENT
-
PROBLEM TO BE SOLVED: To improve Δn of a liquid crystal compound. SOLUTION: One aspect of the present invention is a liquid crystal compound represented by general formula (i) [where Ri1 is a C1 to 15 alkyl group or the like, Ri2 is
- -
-
Paragraph 0169; 0171
(2020/02/28)
-
- Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors
-
The design, synthesis and structure-activity relationships associated with a series of bridged tricyclic pyrimidinone carboxamides as potent inhibitors of HIV-1 integrase strand transfer are described. Structural modifications to these molecules were made in order to examine the effect on potency towards wild-type and clinically-relevant resistant viruses. The [3.2.2]-bridged tricyclic system was identified as an advantageous chemotype, with representatives exhibiting excellent antiviral activity against both wild-type viruses and the G140S/Q148H resistant virus that arises in response to therapy with raltegravir and elvitegravir.
- Patel, Manoj,Naidu, B. Narasimhulu,Dicker, Ira,Higley, Helen,Lin, Zeyu,Terry, Brian,Protack, Tricia,Krystal, Mark,Jenkins, Susan,Parker, Dawn,Panja, Chiradeep,Rampulla, Richard,Mathur, Arvind,Meanwell, Nicholas A.,Walker, Michael A.
-
supporting information
(2020/05/18)
-
- 1-METHYL-4-[(4-PHENYLPHENYL)SULFONYLMETHYL]CYCLOHEXYANOL AND 1-METHYL-4-[[4-(2-PYRIDYL)PHENYL]SULFONYLMETHYL]CYCLOHEXANOL COMPOUNDS AND THEIR THERAPEUTIC USE
-
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted 1-methyl-4-[(4-phenylphenyl)sulfonylmethyl]cyclohexanol and 1-methyl-4-[[4-(2-pyridyl)phenyl]sulfonylme
- -
-
Page/Page column 72; 74
(2020/03/05)
-
- DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
-
Provided herein are dihydropyrimidine derivatives which are useful in the treatment of HBV infection or HBV-induced diseases, as well as pharmaceutical or medical applications thereof.
- -
-
Page/Page column 79
(2019/11/28)
-
- Solid dispersions containing an apoptosis-inducing agent
-
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
- -
-
Page/Page column 257
(2019/03/15)
-
- Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow
-
Cheap and readily available aqueous formaldehyde was used as a formylating reagent in a homologation reaction with nonstabilized diazo compounds, enabled by UV photolysis of bench-stable oxadiazolines in a flow photoreactor. Various aliphatic aldehydes were synthesized along with the corresponding derivatized alcohols and benzimidazoles. No transition-metal catalyst or additive was required to affect the reaction, which proceeded at room temperature in 80 min.
- Chen, Yiding,Leonardi, Marco,Dingwall, Paul,Labes, Ricardo,Pasau, Patrick,Blakemore, David C.,Ley, Steven V.
-
p. 15558 - 15568
(2019/01/04)
-
- PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS
-
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
- -
-
Page/Page column 34
(2018/03/25)
-
- CRYSTAL FORM OF 4H-PYRAZOLO[1,5-alpha]BENZOIMIDAZOLE COMPOUND, PREPARATION METHOD THEREOF AND INTERMEDIATE THEREOF
-
The invention discloses a crystal form A of a compound (I) and a preparation method thereof, and further discloses an application of the crystal form A as a PDE2 or TNF-α inhibitor.
- -
-
Paragraph 0053; 0055
(2018/11/21)
-
- Aminoheteroaryl benzamides as kinase inhibitors
-
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
- -
-
Page/Page column 415; 416
(2016/02/15)
-
- Hydroxypurine compound and use thereof
-
The invention discloses a hydroxypurine compound and a use of the hydroxypurine compound as a PDE2 or TNFa inhibitor and concretely discloses a compound shown in the formula (I) and its tautomer or pharmaceutically acceptable salt.
- -
-
Paragraph 0256; 0260; 0261; 0262
(2016/10/08)
-
- ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
-
Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
- -
-
Paragraph 00375
(2016/04/20)
-
- PYRAZOLE AMIDE DERIVATIVE
-
The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
- -
-
Page/Page column 188; 189
(2015/09/28)
-
- BICYCLIC HETEROARYL DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
-
Bicyclic heteroaryl derivatives of Formula 1, and pharmaceutically acceptable salts, isomers, hydrates and solvates thereof can selectively and effectively inhibit DGAT1, and thus can be useful as medicines for effectively treating dangerous diseases such as obesity, type 2 diabetes, abnormal lipidemia, metabolic syndrome (syndrome X) and the like, which are caused by DGAT1, with no adverse side effects.
- -
-
Page/Page column 24-25
(2013/11/05)
-
- BORON COMPOUND WITH AMINO ACID SKELETON CONTAINING CYCLO RING
-
The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a
- -
-
-
- Discovery of a new class of ghrelin receptor antagonists
-
A series of benzodiazepine antagonists of the human ghrelin receptor GHSR1a were synthesized and their antagonism and metabolic stability were evaluated. The potency of these analogs was determined using a functional aequorin (Euroscreen) luminescent assay measuring the intracellular Ca2+ concentration, and their metabolic stability was measured using an in vitro rat and human S9 hepatocyte assay. These efforts led to the discovery of a potent ghrelin antagonist with good rat pharmacokinetic properties.
- Mihalic, Jeffrey T.,Kim, Yong-Jae,Lizarzaburu, Mike,Deignan, Jeff,Wanska, Malgorzata,Yu, Ming,Fu, Jiasheng,Chen, Xi,Zhang, Alex,Connors, Richard,Liang, Lingming,Lindstrom, Michelle,Ma, Ji,Tang, Liang,Dai, Kang,Li, Leping,Chen, Xiaoqi
-
scheme or table
p. 2046 - 2051
(2012/04/17)
-
- MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
-
The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
- -
-
Page/Page column 195
(2012/11/07)
-
- CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
-
The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
- -
-
Page/Page column 62
(2012/01/03)
-
- LIQUID CRYSTALLINE COMPOUND WITH NEGATIVE DIELECTRIC ANISOTROPY, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY DEVICE
-
A liquid crystal compound is provided that has excellent characteristics, such as a negatively large dielectric anisotropy. A liquid crystal composition containing the compound, and a liquid crystal display device containing the composition are also provi
- -
-
Page/Page column 33
(2011/02/17)
-
- BRIDGED COMPOUNDS AS HIV INTEGRASE INHIBITORS
-
Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, Rs
- -
-
Page/Page column 58
(2010/08/09)
-
- NOVEL COMPOUNDS-300
-
Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4, m, n, q, s, t, X, and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
- -
-
Page/Page column 14
(2009/12/02)
-
- Substituted 4-aminocyclohexane derivatives
-
Substituted 4-aminocyclohexane derivatives having the formula I: [image] wherein R1-R4 are as described herein, methods for their preparation, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted 4-amino
- -
-
Page/Page column 14
(2009/09/07)
-
- Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors
-
Discovery and optimization of a piperidyl benzamide series of 11β-HSD1 inhibitors is described. This series was derived from a cyclohexyl benzamide lead structures to address PXR selectivity, high non-specific protein binding, poor solubility, limited in
- Rew, Yosup,McMinn, Dustin L.,Wang, Zhulun,He, Xiao,Hungate, Randall W.,Jaen, Juan C.,Sudom, Athena,Sun, Daqing,Tu, Hua,Ursu, Stefania,Villemure, Elisia,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
-
scheme or table
p. 1797 - 1801
(2009/12/07)
-
- HIV Integrase Inhibitors
-
The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
- -
-
Page/Page column 82
(2009/10/17)
-
- LIQUID CRYSTAL COMPOUND HAVING NEGATIVE DIELECTRIC ANISOTROPY, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY DEVICE
-
A liquid crystal compound is provided that has excellent characteristics, such as a negatively large dielectric anisotropy. A liquid crystal composition containing the compound, and a liquid crystal display device containing the composition are also provi
- -
-
-
- TETRAHYDROBENZOTHIOPHENE DERIVATIVES
-
Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.
- -
-
Page/Page column 186
(2008/06/13)
-
- DICYCLOALKYL UREA GLUCOKINASE ACTIVATORS
-
Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. (I)
- -
-
Page/Page column 109-110; 130-131
(2008/06/13)
-
- DIFLUOROBENZENE DERIVATIVE AND NEMATIC LIQUID CRYSTAL COMPOSITION MAKING USE OF THE SAME
-
A nematic liquid crystal composition of the present invention includes one or at least two compounds represented by general formula (I) as a first component; and one or at least two compounds represented by general formula (II) as a second component, wherein a dielectric anisotropy is negative. The use of this nematic liquid crystal composition can provide a highly reliable liquid crystal display element capable of maintaining a high voltage-holding ratio even in a high temperature region, and achieving quick responsiveness without reducing the cell gap.
- -
-
Page/Page column 21; 22
(2008/06/13)
-
- UREA GLUCOKINASE ACTIVATORS
-
The invention provides a compound of general formula (I) wherein the substituents are defined futher in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds
- -
-
Page/Page column 74-75; 103-104
(2008/06/13)
-
- Benzimidazole compound
-
An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.
- -
-
Page/Page column 93
(2008/06/13)
-
- ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
-
The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
- -
-
Page/Page column 207-208
(2008/06/13)
-
- BICYCLIC DERIVATIVES AS CETP INHIBITORS
-
The present invention relates to novel compounds of formula (I): or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay
- -
-
Page/Page column 86; 87
(2008/06/13)
-
- Novel Angiogenesis inhibitors and pharmaceutical/cosmetic applications thereof
-
Novel derivatives of fumagalone have the general formula (I): and are useful angiogenes is inhibitors; these can be formulated into pharmaceutical compositions suited for human or veterinary medicine, or can be formulated into cosmetic compositions.
- -
-
Page/Page column 7; sheet 2
(2010/11/27)
-
- New bioorganic reagents: Evolved cyclohexanone monooxygenase - Why is it more selective?
-
Four mutants of the cyclohexanone monooxygenase (CHMO) evolved as catalysts for Baeyer-Villiger oxidation of 4-hydroxycyclohexanone were investigated as catalysts for a variety of 4-substituted and 4,4-disubstituted cyclohexanones. Several excellent catalytic matches (mutant/substrate) were identified. The most important, however, is the finding that, in a number of cases, a mutant with a single exchange, Phe432Ser, was shown to be as robust and more selective as a catalyst than the wild-type CHMO. All biotransformations were performed on a laboratory scale, allowing full characterization of the products. The absolute configurations of two products were established. A model suggesting a possible role of the 432 serine residue in enantioselectivity control is proposed.
- Kayser, Margaret M.,Clouthier, Christopher M.
-
p. 8424 - 8430
(2007/10/03)
-
- 3-AMINO-PYRAZOLO[3,4B]PYRIDINES USED AS INHIBITORS OF PROTEIN TYROSINE KINASES FOR TREATING ANGIOGENIC, HYPERPROLIFERATIVE OR NEURODEGENERATIVE DISEASES
-
The invention relates to compounds of general formula (I), in which R1 and R2 are described in the application, to the use of the compounds of general formula (I) as inhibitors of protein tyrosine kinases for treating various diseases, and to the compounds of general formulas (II) and (III) as intermediate compounds for producing compounds of general formula (I), in which X, R1a and R2a have the meanings as described in general formulas (II) and (III).
- -
-
Page/Page column 49
(2008/06/13)
-
- New high affinity H3 receptor agonists without a basic side chain
-
In this study, we replaced the basic amine function of the known histamine H3 receptor agonists imbutamine or immepip with non-basic alcohol or hydrocarbon moieties. All compounds in this study show a moderate to high affinity for the cloned human H3 receptor and, unexpectedly, almost all of them act as potent agonists. Moreover, in the alcohol series, we consistently observed an increased selectivity for the human H3 receptor over the human H4 receptor, but none of the compounds in this series possess increased affinity and functional activity compared to their alkylamine congeners. In this new series of compounds VUF5657, 5-(1H-imidazol-4-yl)-pentan-1-ol, is the most potent histamine H3 receptor agonist (pKi = 8.0 and pEC50 = 8.1) with a 320-fold selectivity at the human H3 receptor over the human H 4 receptor.
- Kitbunnadaj, Ruengwit,Hoffmann, Marcel,Fratantoni, Silvina A.,Bongers, Gerold,Bakker, Remko A.,Wieland, Kerstin,El Jilali, Ahmed,De Esch, Iwan J. P.,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
-
p. 6309 - 6323
(2007/10/03)
-
- Total synthesis of cis and trans-hydroxyglimepiride: Active metabolite of glimepiride
-
Syntheses of trans-hydroxyglimepiride 2b, a human metabolite of the blood glucose lowering agent glimepiride 1 and its corresponding cis-stereoisomer 2a, are described.
- Gurjar, Mukund K.,Joshi, Ramesh A.,Chaudhuri, Siddhartha R.,Joshi, Shreerang V.,Barde, Anup R.,Gediya, Lalji K.,Ranade, Prasad V.,Kadam, Suresh M.,Naik, Sanjay J.
-
p. 4853 - 4855
(2007/10/03)
-
- Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
-
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
- -
-
-
- Novel bicyclic lactam inhibitors of thrombin: Potency and selectivity optimization through P1 residues
-
Peptidomimetic inhibitors of thrombin lacking the important Ser195-carbonyl interaction have been prepared. The binding energy lost after the removal of the activated carbonyl was recaptured through a series of modifications of the P1 residues of the bicyclic lactam inhibitors. Selected substituted compounds displayed useful pharmacological profiles both in vitro and in vivo.
- Levesque, Sophie,St-Denis, Yves,Bachand, Benoit,Preville, Patrice,Leblond, Lorraine,Winocour, Peter D,Edmunds, Jeremy J,Rubin,Siddiqui
-
p. 3161 - 3164
(2007/10/03)
-
- A synthesis of (±)-stemodinone: An application of organoiron chemistry to the construction of sterically congested quaternary carbon centers
-
A synthesis of racemic stemodinone is described, using tricarbonyl(1-5- η-4-methoxy-1,3-dimethylcyclohexadienyl)iron(I) hexafluorophosphate (9) as an electrophile that is the A-ring precursor. Reaction of 9 with the tin enolate from 4,4-(ethylenedioxy)cyclohexanecarbaldehyde proceeded with excellent regioselectivity and high yield to generate an intermediate representing the A and C rings of the target molecule. The B ring was constructed by introducing a two-carbon electrophilic group onto the A ring, followed by ring closure using an intramolecular enolate alkylation. Installation of the D ring and manipulation to give the final product followed transformations precedented with this series of compounds.
- Pearson, Anthony J.,Fang, Xinqin
-
p. 5284 - 5292
(2007/10/03)
-
- Stereoselective Cyclization of 4-Substituted 5-Hexen-1-ols and Related Compounds by Benzeneselenenyl Triflate
-
Oxyselenylation of 4-substituted 5-hexen-1-ols 1 with benzeneselenenyl trifluoromethanesulfonate proceeds by intramolecular exo cyclization stereoselectively to give 3-substituted trans- or cis-2-(phenylselenenylmethyl)tetrahydropyrans 3.Formation of the trans isomers is favored when the substituents contain alkyl or phenyl substituents in the 4-position, whereas the cis isomers predominate when the substituents are alkoxyalkyl, alkoxyl, acyl, and hydroxyl.The mechanism of the trans and cis stereoselectivity is explained by steric and electronic effects in the phenylseleniranium intermediates, 7 and 8. - Key Words: Oxyselenenylation / Benzeneselenenyl triflate / Selenium compounds / Trifluoromethanesulfonate / Alkenols
- Inoue, Hirohumi,Murata, Shizuaki,Suzuki, Toshiyasu
-
p. 901 - 910
(2007/10/02)
-
- Substituted Benzamides with Conformationally Restricted Side Chains. 5. Azabicyclo Derivatives as 5-HT4 Receptor Agonists and Gastric Motility Stimulants
-
The syntheses of benzamides containing azabicyclo side chains and their 5-HT4 receptor agonist and 5-HT3 receptor antagonist properties are described.These compounds were designed to mimic higher energy conformations of quinol
- King, Frank D.,Hadley, Michael S.,Joiner, Karen T.,Martin, Roger T.,Sanger, Gareth J.,et al.
-
p. 683 - 689
(2007/10/02)
-
- Dialkyl-substituted dithianes and pesticidal compositions
-
The present invention provides compounds of the formula (I): STR1 wherein m and n are independently selected from 0, 1 or 2, STR2 R is selected from hydrogen, methyl or ethyl; R1 is selected from C1-4 hydrocarbyl substituted by one to five halo atoms, and a group --C C--R9 wherein R9 is a group S(O)w --R10 wherein R10 is trifluoromethyl, methyl or ethyl and w is 0, 1 or 2 or R9 is a C3-5 aliphatic group or an aliphatic group containing up to 5 carbon atoms atoms substituted by C1-4 alkoxy, C2-6 alkoxyalkoxy, C1-8 acyloxy, halo or hydroxy, a group COR11 wherein R11 is hydrogen, C1-4 alkyl, C1-4 alkoxy or a group NR12 R13 wherein R12 and R13 are independently selected from hydrogen, methyl or ethyl, or R9 is SiR14 R15 R16 wherein R14 to R16 are the same or different and each is a C1-4 aliphatic group or R14 and R15 are C1-4 aliphatic groups and R16 is a phenyl group; R2, R3, R7 and R8 are independently selected from hydrogen, methyl or halo; R4a and R4b, R6a and R6b are independently selected from hydrogen, C1-3 alkyl, C2-3 alkenyl or alkynyl each being optionally substituted by halo, cyano or C1-4 alkoxy; cyano, halo or a group COR 11a wherein R11a is hydrogen, C1-4 alkoxy, C1-4 alkyl or a group NR12a R13a wherein R12a and R13a are independently selected from hydrogen, methyl or ethyl; R5a is a non-aromatic hydrocarbyl group containing up to seven carbon atoms, or phenyl each optionally substituted by cyano, halo, C1-4 alkyl, C1-4 haloalkyl, C3-4 cycloalkyl, C1-4 alkoxy or a group S(O)q R17 wherein q is 0, 1 or 2 and R17 is methyl or ethyl and R5b is hydrogen, hydroxy or C1-4 alkyl optionally substituted by alkoxy; and represents --CH--CH-- or --C=C-- which are useful pesticides, processes for their preparation, pesticidal formulations containing them and their use in the control or prevention of pest infestation.
- -
-
-
- A Photochemical Approach to the Taxanes
-
The de Mayo sequence has been applied to the inter- and intramolecular photocycloaddition of various cycloalkenes with homocamphorquinone derivatives to generate a model for the A, B, and C rings of the taxanes.A model sequence of reactions applicable to
- Berkowitz, W. F.,Amarasekara, A. S.,Perumattam, J. J.
-
p. 1119 - 1124
(2007/10/02)
-
- 99.Transferts d'hydrogenes dans les cations radicaux ethylene-acetals derives de cyclopentanones et cyclohexanones
-
Hydrogen Transfer during Decompositions of Molecular Ions of Acetals Derived from Substituted Cyclopentanones and Cyclohexanones.The isomerisation process of ethylene-acetal radical ions of low internal energy has been reinvestigated in more detail .The ring contraction of cyclohexane derivatives into methylcyclopentanes is quite general for these ions.The relative rates of H transfers to the C free resulting from C-C cleavage α to the acetal group plays the most important part in the mechanism.
- Audier, H. E.,Tabet, J. C.,Fetizon, M.
-
p. 903 - 911
(2007/10/02)
-
- A Photochemical Approach to the Taxanes
-
The de Mayo sequence has been applied to the inter- and intramolecular photocycloaddition of various cycloalkenes with homocamphorquinone derivatives to generate a model for the A, B and C rings of the Taxanes.
- Berkowitz, W. F.,Perumattam, J.,Amarasekara, A.
-
p. 3665 - 3668
(2007/10/02)
-
- Thiazolidine derivatives and production thereof
-
A thiazolidine derivative of the general formula, STR1 is a cyclohexane ring having an oxo or hydroxyl group as a substituent on any of the methylene groups constituting the ring and R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms,
- -
-
-
- Sulphur participation in cyclization reactions
-
Cyclization initiated by thiiranium ions was investigated.Cis-fused decalins were formed by a process involving inversion.In nitromethane a sulphonium salt 8 was formed.The reactions of 8 with nucleophilic reagent deviated from those of comparable compoun
- Loos, Walter A. J. de,Kuijk, Anne J. W. van den Berg-van,Iersel, Hans M. van,Haan, Jan W. de,Buck, Henk M.
-
-