- The synthesis of a 5HT2C receptor agonist
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This report describes the large-scale synthesis of 1 that features a Fischer indole strategy to form an advanced intermediate followed by reduction to the indoline to construct the tetracyclic core of the molecule. Resolution using dibenzoyl-D-tartaric acid affords access to a single enantiomer, from which a Suzuki coupling builds in the biaryl functionality. Deprotection followed by salt formation furnishes the desired target molecule.
- Hobson, Lindsay A.,Nugent, William A.,Anderson, Stephen R.,Deshmukh, Subodh S.,Haley III, James J.,Liu, Pingli,Magnus, Nicholas A.,Sheeran, Patrick,Sherbine, James P.,Stone, Benjamin R. P.,Zhu, Jiang
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Read Online
- InBr3- and AgOTf-catalyzed beckmann rearrangement of (E)-benzoheterocyclic oximes
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Beckmann rearrangement of (E)-4-chromanone oxime, (E)-5-oximino-3,4- dihydro-1(2H)-benzoxepines, and (E)-5-oximino-3,4-dihydro-1(2H)-benzothiepine are catalyzed by InBr3 and AgOTf in refluxing acetonitrile resulting in the formation of pharmaceutically active heterocycles benzoxazepin-4-one, 5-oxo-benzoxazocines, and 5-oxo-benzothiazocine derivative, respectively, in excellent yield. Copyright
- Tandon, Vishnu K.,Awasthi, Anoop K.,Maurya, Hardesh K.,Mishra, Pushyamitra
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Read Online
- Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents
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Three series of bitopic benzopyranomorpholine analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined using the method of radioligand binding assay. Most compounds demonstrated considerable binding affinities and selectivity for D3 receptor. Besides, the compounds were screened for their ability to alleviate withdrawal symptoms of opioid addiction in animal behavioral models. The results showed that compound 20h displayed nanomolar affinity for the D3R, and exhibited anti-drug addiction efficacy in the animal model of of naloxone-induced withdrawal symptoms in morphine-dependent mice.
- Cai, Jin,Chen, Xixi,Huang, Mingqi,Ji, Min,Wang, Yuhong
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- Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction
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Histone deacetylase 6 (HDAC6) has become a promising therapeutic target for central nervous system diseases due to its more complex protein structure and biological functions. However, low brain penetration of reported HDAC6 inhibitors limits its clinical application in neurological disorders. Therefore, the benzazepine, a brain-penetrant rigid fragment, was utilized to design a series of selective HDAC6 inhibitors to improve brain bioavailability. Various synthetic strategies were applied to assemble the tetrahydro-benzazepine ring, and 22 compounds were synthesized. Among them, compound 5 showed low nanomolar potency and strong isozyme selectivity for the inhibition of HDAC6 (IC50 = 1.8 nM, 141-fold selectivity over HDAC1) with efficient binding patterns like coordination with the zinc ion and π-π stacking effect. Western blot results showed it could efficiently transport into SH-SY5Y cells and selectively enhance the acetylation level of α-tubulin with a moderate effect on Histone H3. Notably, pharmacokinetic studies demonstrated that compound 5 (brain/plasma ratio of 2.30) had an excellent ability to penetrate the blood-brain barrier of C57 mice. In male rats with transient middle cerebral artery occlusion (MCAO), compound 5 significantly reduced the cerebral infarction from 21.22% to 11.47% and alleviated neurobehavioral deficits in post-ischemic treatment, which provided a strong rationale for pursuing HDAC6-based therapies for ischemic stroke.
- Guo, Zheng,Zhang, Zixue,Zhang, Yi,Wang, Guan,Huang, Ziyi,Zhang, Qinwei,Li, Jianqi
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- Access to multi-functionalized oxazolines via silver-catalyzed heteroannulation of enamides with sulfoxonium ylides
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Disclosed herein is an efficient Ag-catalyzed [4 + 1] heteroannulation reaction of enamides with α-carbonyl sulfoxonium ylides. The diastereoselective transformation provides a practical access to a diverse range of multi-functionalized oxazoline derivatives. The synthetic utility of the resultant tetra-substituted oxazolines is further demonstrated by a series of useful manipulations into valuable building blocks of pharmaceutical relevance.
- Liu, Rui-Hua,Shan, Qi-Chao,Gao, Ya,Loh, Teck-Peng,Hu, Xu-Hong
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supporting information
p. 1411 - 1414
(2020/10/29)
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- [1,5]-Hydride shift-cyclization versus C(sp2)-H functionalization in the knoevenagel-cyclization domino reactions of 1,4- And 1,5-Benzoxazepines
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Domino cyclization reactions of N-aryl-1,4- and 1,5-benzoxazepine derivatives involving [1,5]-hydride shift or C(sp2)-H functionalization were investigated. Neuroprotective and acetylcholinesterase activities of the products were studied. Domino Knoevenagel-[1,5]-hydride shift-cyclization reaction of N-aryl-1,4-benzoxazepine derivatives with 1,3-dicarbonyl reagents having active methylene group afforded the 1,2,8,9-tetrahydro-7bH-quinolino [1,2-d][1,4]benzoxazepine scaffold with different substitution pattern. The C(sp3)-H activation step of the tertiary amine moiety occurred with complete regioselectivity and the 6-endo cyclization took place in a complete diastereoselective manner. In two cases, the enantiomers of the chiral condensed new 1,4-benzoxazepine systems were separated by chiral HPLC, HPLC-ECD spectra were recorded, and absolute configurations were determined by time-dependent density functional theory- electronic circular dichroism (TDDFT-ECD) calculations. In contrast, the analogue reaction of the regioisomeric N-aryl-1,5-benzoxazepine derivative did not follow the above mechanism but instead the Knoevenagel intermediate reacted in an SEAr reaction [C(sp2)-H functionalization] resulting in a condensed acridane derivative. The AChE inhibitory assays of the new derivatives revealed that the acridane derivative had a 6.98 μM IC50 value.
- Antus, Sándor,Buglyó, Balázs,Chen, Yinghan,Kiss-Szikszai, Attila,Kurtán, Tibor,Li, Dehai,Mándi, Attila,Mátyus, Péter,Tóth, László,Tao, Lingxue,Vargáné, Dóra Szalóki,Zhang, Haiyan
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- Diphenyliodonium Ion/Et3N Promoted Csp2-H Radical Phosphorylation of Enamides
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This work reports a simple and efficient method for the direct phosphorylation of enamide under metal-free conditions. The P-centered radicals, derived from secondary phosphine oxides, are generated under mild reaction conditions in the presence of diphenyliodonium salt and Et3N and are introduced onto a range of enamides in good isolated yields. The method features broad substrate scope, good functional group tolerance, and efficient scale-up.
- Pal, Suman,Gaumont, Annie-Claude,Lakhdar, Sami,Gillaizeau, Isabelle
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supporting information
p. 5621 - 5625
(2019/08/01)
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- The ruthenium-catalyzed C-H functionalization of enamides with isocyanates: Easy entry to pyrimidin-4-ones
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Ruthenium-catalyzed heteroannulation between enamides and isocyanates has been realized as a complementary approach to conventional strategies for the synthesis of pyrimidin-4-ones. High step-A nd atom-economy was achieved for the rapid construction of such privileged scaffolds, which are found in a multitude of pharmaceutical compounds. The generality and practicability of this transformation were reflected by the broad scope of substrates with diverse functional groups, large-scale synthesis, and late-stage diversification.
- Shi, Pengfei,Li, Song,Hu, Lu-Min,Wang, Cong,Loh, Teck-Peng,Hu, Xu-Hong
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supporting information
p. 11115 - 11118
(2019/09/20)
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- Directing group assisted nucleophilic substitution of propargylic alcohols via o -quinone methide intermediates: Br??nsted acid catalyzed, highly enantio- and diastereoselective synthesis of 7-alkynyl-12a-acetamido-substituted benzoxanthenes
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BINOL-based, chiral phosphoric acids catalyze the substitution of 1-(o-hydroxyphenyl)propargylic alcohols with enamides to furnish 7-alkynyl-12a-acetamido-substituted benzo[c]xanthenes and related heterocycles in a one-pot operation with excellent diastereo- and enantioselectivity. Ambient reaction temperature, operationally simple reaction conditions, low catalyst loading, high yields, and excellent stereocontrol are attractive features of this process and make it a highly practical and versatile transformation.
- Saha, Satyajit,Schneider, Christoph
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supporting information
p. 648 - 651
(2015/03/05)
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- One-Pot preparation of 2-arylbenzofurans from oximes with diaryliodonium triflate
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A variety of 2-arylbenzofurans were obtained in good yields by the O-arylation of oximes with diaryliodonium triflates, followed by the treatment with HCl in dioxane under warming conditions through the [3,3]-sigmatropic reaction. The present reaction is one-pot transition metal-free method for the preparation of various 2-arylbenzofurans from oximes, which are easily available from the reaction of alkyl aryl ketones with hydroxylamine.
- Miyagi, Kotaro,Moriyama, Katsuhiko,Togo, Hideo
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p. 2122 - 2136
(2015/01/09)
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- Rhodium(iii)-catalyzed olefinic C-H alkynylation of enamides at room temperature
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Rh(iii)-catalyzed C-H olefinic alkynylation of enamides for the stereospecific construction of synthetically useful Z-type enynamides is reported. This protocol displays good functionality tolerance and operational simplicity thus providing an alternative synthetic opportunity for the ease of access to specific 1,3-enyne derivatives.
- Feng, Chao,Feng, Daming,Loh, Teck-Peng
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supporting information
p. 9865 - 9868
(2014/08/18)
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- 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
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The present invention relates to novel triazolo [4,3-a]pyridine derivatives of Formula (I), wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ("mGluR2"), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
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Page/Page column 49
(2012/05/31)
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- Decarboxylative acylation of cyclic enamides with α-oxocarboxylic acids by palladium-catalyzed C-H activation at room temperature
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An efficient catalytic decarboxylative acylation of unactivated sp 2 (alkenyl) C-H bonds has been developed. Various substituted α-oxocarboxylic acids with different electronic properties react under mild conditions to afford a diverse range of β-acyl enamide products in good yields. The reaction is proposed to proceed via a cyclic vinylpalladium intermediate, facilitating the decarboxylative dehydrogenative process with enamide coupling partners.
- Wang, Hua,Guo, Li-Na,Duan, Xin-Hua
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supporting information
p. 4358 - 4361
(2012/10/29)
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- Metal-Free 2,2,6,6-tetramethylpiperidin-1-yloxy radical (TEMPO) catalyzed aerobic oxidation of hydroxylamines and alkoxyamines to oximes and oxime ethers
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TEMPO-Mediated oxidation of hydroxylamines (=hydroxyamines) and alkoxyamines to the corresponding oxime derivatives is reported (TEMPO=2,2,6,6-tetramethylpiperidin-1-yloxy radical; Scheme 2). These environmentally benign oxidations proceed in good to excellent yields (Table 1). For alkoxyamines, oxidation to the corresponding oxime ethers can be performed by using dioxygen as a terminal oxidant in the presence of 5-10 mol-% of TEMPO or 4-substituted derivatives thereof as a catalyst (Scheme 3 and Table 2). Importantly, benzyl bromides can directly be transformed to oxime ethers via in situ alkoxyamine formation by a nucleophilic substitution followed by TEMPO-mediated oxidation (Scheme 4 and Table 3). Copyright
- Wertz, Sebastian,Studer, Armido
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p. 1758 - 1772,15
(2012/12/13)
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- The application of the schmidt reaction and beckmann rearrangement to the synthesis of bicyclic lactams: Some mechanistic considerations
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The syntheses of some methoxy-substituted bicyclic lactams, of the types 3 and 4, are reported employing two different conditions for the Schmidt reaction of appropriate ketones and employing two different conditions for the Beckmann rearrangement of the corresponding ketoximes. The alkyl to aryl migration ratios of the reactions were determined by high-performance liquid chromatography analysis of the reactions. The mechanisms of the reactions reported are discussed, some limitations of the reported mechanisms identified, and an alternative mechanism proposed in light of the outcomes of the various reactions. Application of the Schmidt reaction and Beckmann rearrangement was used for the synthesis of some chloro bicyclic lactams, of the types 3 and 4. CSIRO 2010.
- Crosby, Ian T.,Shin, James K.,Capuano, Ben
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experimental part
p. 211 - 226
(2011/06/21)
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- Regioselective synthesis of heterocycles containing nitrogen neighboring an aromatic ring by reductive ring expansion using diisobutylaluminum hydride and studies on the reaction mechanism
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(Chemical Equation Presented) A systematic investigation of the reductive ring-expansion reaction of cyclic ketoximes fused to aromatic ringswith diisobutylaluminum hydride (DIBALH) is described. This reaction regioselectively afforded a variety of five- to eight-membered bicyclic heterocycles or tricyclic heterocycles containing nitrogen neighboring an aromatic ring, including indoline, 1,2,3,4,5,6-hexahydrobenz[b]azocine, 3,4-dihydro-2H-benzo[b] [1,4]oxazine, 2,3,4,5-tetrahydrobenzo[b][1,4]thiazepine, 1,2,3,4,5,6- hexahydroazepino[3,2-b]-indole, 2,3,4,5-tetrahydro-1H-benzothieno[2,3-b]azepine, 2,3,4,5-tetrahydro-1H-benzothieno[3,2-b]-azepine, 5,6-dihydrophenanthridine, and 5,6,11,12-tetrahydrodibenz[b, f]azocine. The reaction mechanism leading to the rearrangement was investigated on the basis of the restricted Becke three-parameter plus Lee-Yang-Parr (B3LYP) density functional theory (DFT) with the 6-31G (d) basis set. It was found that the reaction proceeds through a three-centered transition state via a stepwise mechanism because the potential energy curve along the intrinsic reaction coordinate (IRC) had twomaxima (saddle points; TS1 and TS2) and the partial phenonium cation intermediate C. In addition to cyclic ketoximes fused to aromatic rings, the reactions of various cyclic and acyclic ketoximeswere examined to investigate preference of migrating group. It was found that themore electron-rich group migrated preferentially to give the corresponding secondary amines.
- Cho, Hidetsura,Iwama, Yusuke,Sugimoto, Kenji,Mori, Seiji,Tokuyama, Hidetoshi
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experimental part
p. 627 - 636
(2010/04/29)
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- Regiospecific synthesis of unsubstituted basic skeletons of heterocycles containing nitrogen neighboring an aromatic ring by the reductive ring expansion reaction using diisobutylaluminum hydride
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A systematic investigation of reductive ring expansion reaction of oximes with diisobutylaluminum hydride (DIBAH) was performed. The reaction regiospecifically provided a variety of unsubstituted bicyclic heterocycles 3a-3g or tricyclic heterocycles 3h, 3j-3l that contained nitrogen attached to an aromatic ring.
- Cho, Hidetsura,Iwama, Yusuke,Sugimoto, Kenji,Kwon, Eunsang,Tokuyama, Hidetoshi
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experimental part
p. 1183 - 1190
(2009/11/30)
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- Direct arylation of cyclic enamides via Pd(ii)-catalyzed C-H activation
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A new direct coupling of cyclic enamides with aryl boronic acids via Pd(ii)-catalyzed C-H functionalization has been achieved with good yields (up to 90%).
- Zhou, Hai,Chung, Wan-Jun,Xu, Yun-He,Loh, Teck-Peng
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supporting information; experimental part
p. 3472 - 3474
(2009/12/07)
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- 2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors
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A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-γ (INF-γ) production.
- Cole, Andrew G.,Bohnstedt, Adolph C.,Paradkar, Vidyadhar,Kingsbury, Celia,Quintero, Jorge G.,Park, Haengsoon,Lu, Yingchun,You, Ming,Neagu, Irina,Diller, David J.,Letourneau, Jeffrey J.,Shao, Yuefei,James, Ray A.,Riviello, Christopher M.,Ho, Koc-Kan,Lin, Tsung H.,Wang, Bojing,Appell, Kenneth C.,Sills, Matthew,Quadros, Elizabeth,Kimble, Earl F.,Ohlmeyer, Michael H.J.,Webb, Maria L.
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scheme or table
p. 6788 - 6792
(2010/06/12)
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- Highly enantioselective borane reduction of heteroaryl and heterocyclic ketoxime ethers catalyzed by novel spiroborate ester derived from diphenylvalinol: Application to the synthesis of nicotine analogues
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(Chemical Equation Presented) An asymmetric synthesis for the preparation of nonracemic amines bearing heterocyclic and heteroaromatic rings is described. A variety of important enantiopure thionyl and arylalkyl primary amines were afforded by the borane-mediated enantioselective reduction of O-benzyl ketoximes using 10% of catalyst 10 derived from (S)-diphenylvalinol and ethylene glycol with excellent enantioselectivity, in up to 99% ee. The optimal condition for the first asymmetric reduction of 3- and 4-pyridyl-derived O-benzyl ketoxime ethers was achieved using 30% of catalytic loading in dioxane at 10°C. (S)-N-ethylnornicotine (3) was also successfully synthesized from the TIPS-protected (S)-2-amino-2-pyridylethanol in 97% ee.
- Huang, Kun,Merced, Francisco G.,Ortiz-Marciales, Margarita,Melendez, Hector J.,Correa, Wildeliz,De Jesus, Melvin
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p. 4017 - 4026
(2008/09/21)
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- GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
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(2008/12/04)
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- New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists
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Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desired. However, its peptidic nature limits its bioavailability. We report herein the discovery of potent, nonpeptidic, benzylurea derived agonists of the vasopressin V2 receptor. We describe substitutions on the benzyl group to give improvements in potency and subsequent modifications to the urea end group to provide improvements in solubility and increased oral efficacy in a rat model of diuresis. The lead compound 20e (VA106483) is reported for the first time and has been selected for clinical development.
- Yea, Christopher M.,Allan, Christine E.,Ashworth, Doreen M.,Barnett, James,Baxter, Andy J.,Broadbridge, Janice D.,Franklin, Richard J.,Hampton, Sally L.,Hudson, Peter,Horton, John A.,Jenkins, Paul D.,Penson, Andy M.,Pitt, Gary R. W.,Rivière, Pierre,Robson, Peter A.,Rooker, David P.,Semple, Graeme,Sheppard, Andy,Haigh, Robert M.,Roe, Michael B.
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supporting information; experimental part
p. 8124 - 8134
(2009/11/30)
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- 2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS
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A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
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(2008/06/13)
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- Carbocyclization by radical closure onto O-trityl oximes: Dramatic effect of diphenyl diselenide
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O-Trityl oximes of 5- and 6-iodoaldehydes undergo radical cyclization to produce oximes when treated in refluxing tetrahydrofuran (THF) with Bu 3SnH, 1,1′-azobis(cyclohexanecarbonitrile), i-Pr 2NEt, and diphenyl diselenide (PhSeSePh).
- Clive, Derrick L. J.,Pham, Mai P.,Subedi, Rajendra
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p. 2713 - 2717
(2007/10/03)
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- Piperazine derivatives and methods of use
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Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 39
(2008/06/13)
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- Cyclic amine derivatives and methods of use
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Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 39
(2010/02/14)
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- BICYCLIC COMPOUNDS HAVING BRADYKININ RECEPTORS AFFINITY AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and
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- Amino-1,3,5-triazines N-substituted with chiral bicyclic radicals, process for their preparation, compositions thereof, and their use as herbicides and plant growth regulators
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Amino-1,3,5-triazines N-substituted with chiral bicyclic radicals, process for their preparation, compositions thereof, and their use as herbicides and plant growth regulators. The invention relates to an optically active compound of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to proceses for their preparation, to compositions thereof, and to their use as herbicides or plant growth regulators. The invention also relates to novel intermediates of formula (III), (V) and (XIII) as defined in the description.
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- CYCLIC AMINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF INFLAMMATION-RELATED DISORDERS MEDIATED BY BRADYKININ
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Compounds of formula (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation mediated by Bradykinin. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes wherein q, t, R, Ra, Rb, Rc and R2 are as defined herein.
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Page 111; 112
(2010/02/09)
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- Substituted aryl 1,4-pyrazine derivatives
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Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
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- Phenoxyalkylamines in Semi-rigid Conformation: Synthesis & Pharmacological Activity of N1-(4'-Chromanyl)-N4-arylpiperazines & N1-(2'-Chromanylmethyl)-N4-arylpiperazines
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Synthesis and pharmacological activity of N1-(4'-chromanyl)-N4-arylpiperazines and N1-(chromanylmethyl)-N4-arylpiperazines, cyclic congeners of N1-aryloxyalkyl-N4-arylpiperazines, are reported.None of the compounds of this series shows any significant pharmacological activity.
- Pratap, Ram,Gupta, R. C.,Anand, Nitya
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p. 1063 - 1067
(2007/10/02)
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- New method for controlling fungi using 4-chromone, 4-chromanone, 4-chromone oxime and 4-chromanone oxime compounds
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Certain 4-chromones, 4-chromanones, 4-chromone oximes, and 4-chromanone oximes have been found to be active against fungi. These generally well-known compounds can be applied to seeds, plants, animals, objects, or places for preventing damage due to fungi
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