cas 771-99-3, 4-Phenylpiperidine | Articles data

Articles about 771-99-3Total 40 be found

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Method for preparing piperidine compound by reducing pyridine compound through hydrogen transfer
The invention discloses a method for preparing a piperazine compound through a hydrogen transfer reduction of a pyridine compound, belonging to the field of organic synthesis. Under mild conditions, pyridine derivatives are used as raw materials, oxazolidine is used as a hydrogen transfer reagent, and cheap transition metals such as copper, cobalt, silver, palladium and the like are used as catalysts for catalysis of a hydrogen transfer reaction on 1,2,3,4-substitution sites, so a series of hydrogen transfer reduction product piperidine compounds are prepared, wherein the oxazaborolidine is obtained by a reaction of amino acid with a tetrahydrofuran complex of borane. The method has the advantages that product yield is high, reaction conditions are mild, the general applicability of raw materials is good, a hydrogen transfer reagent is cheap and easy to obtain, and good reproducibility can still be shown after quantitative reaction is conudcted. Therefore, the method of the invention provides an effective scheme for the industrial production of other high-value compounds containing the structure in the future.
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Paragraph 0032; 0033; 0034; 0035; 0036

(2021/04/28)

Synthetic method of 4 -phenyl piperidine hydrochloride
The invention discloses a synthesis method of 4 -phenylpiperidine hydrochloride, and the route is as shown in the specification. The method has the advantages of cheap and easily available raw materials, simple operation and post-treatment, high yield, high product purity and the like, and is suitable for industrial production.
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(2021/11/06)

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor
Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side effects (EPSs) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with contrasting kinetic profiles. Haloperidol displays fast association/slow dissociation at the D2R, whereas clozapine exhibits relatively slow association/fast dissociation. Recently, we have provided evidence that slow dissociation from the D2R predicts hyperprolactinemia, whereas fast association predicts EPS. Unfortunately, clozapine can cause severe side effects independent of its D2R action. Our results suggest an optimal kinetic profile for D2R antagonist APDs that avoids EPS. To begin exploring this hypothesis, we conducted a structure-kinetic relationship study of haloperidol and revealed that subtle structural modifications dramatically change binding kinetic rate constants, affording compounds with a clozapine-like kinetic profile. Thus, optimization of these kinetic parameters may allow development of novel APDs based on the haloperidol scaffold with improved side-effect profiles.
Fyfe, Tim J.,Kellam, Barrie,Sykes, David A.,Capuano, Ben,Scammells, Peter J.,Lane, J. Robert,Charlton, Steven J.,Mistry, Shailesh N.
p. 9488 - 9520
(2019/11/11)

Cobalt-bridged secondary building units in a titanium metal-organic framework catalyze cascade reduction of N-heteroarenes
We report here a novel Ti3-BPDC metal-organic framework (MOF) constructed from biphenyl-4,4′-dicarboxylate (BPDC) linkers and Ti3(OH)2 secondary building units (SBUs) with permanent porosity and large 1D channels. Ti-OH groups from neighboring SBUs point toward each other with an O-O distance of 2 ?, and upon deprotonation, act as the first bidentate SBU-based ligands to support CoII-hydride species for effective cascade reduction of N-heteroarenes (such as pyridines and quinolines) via sequential dearomative hydroboration and hydrogenation, affording piperidine and 1,2,3,4-tetrahydroquinoline derivatives with excellent activity (turnover number ～ 1980) and chemoselectivity.
Feng, Xuanyu,Song, Yang,Chen, Justin S.,Li, Zhe,Chen, Emily Y.,Kaufmann, Michael,Wang, Cheng,Lin, Wenbin
p. 2193 - 2198
(2019/02/20)

Modulators of protease activated receptors
The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for therapies such as metabolic syndrome, obesity, type II diabetes, fibrosis and cardiovascular diseases, whether they are used alone or in combination with other treatment modalities.
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(2018/02/20)

Direct Palladium-Catalyzed β-Arylation of Lactams
A direct and catalytic method is reported here for β-arylation of N-protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium-catalyzed desaturation, Ar?X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
Chen, Ming,Liu, Feipeng,Dong, Guangbin
supporting information
p. 3815 - 3819
(2018/03/13)

Hydrogenation of Pyridines Using a Nitrogen-Modified Titania-Supported Cobalt Catalyst
Novel heterogeneous catalysts were prepared by impregnation of titania with a solution of cobalt acetate/melamine and subsequent pyrolysis. The resulting materials show an unusual nitrogen-modified titanium structure through partial implementation of nitrogen into the support. The optimal catalyst displayed good activity and selectivity for challenging pyridine hydrogenation under acid free conditions in water as solvent.
Chen, Feng,Li, Wu,Sahoo, Basudev,Kreyenschulte, Carsten,Agostini, Giovanni,Lund, Henrik,Junge, Kathrin,Beller, Matthias
supporting information
p. 14488 - 14492
(2018/10/26)

2,2,6,6-Tetramethylpiperidin-1-yloxycarbonyl: A Protecting Group for Primary, Secondary, and Heterocyclic Amines
The 2,2,6,6-tetramethylpiperidin-1-yloxycarbonyl (Tempoc) protecting group is readily introduced by the reaction of amines with a new acyl transfer reagent, 4-nitrophenyl (2,2,6,6-tetramethylpiperidin-1-yl) carbonate (NPTC). Tempoc has a reactivity profile that complements the commonly used t-butyloxycarbonyl (Boc) and benzyloxycarbonyl (Cbz) protecting groups. Deprotection can be achieved under mild reductive conditions with in situ generated Cu(I) species or by thermolytic cleavage at 135 °C. Mechanistic studies on the deprotection of Tempoc-indole suggest a combination of ionic and radical fragmentation pathways under thermal conditions.
Lizza, Joseph R.,Bremerich, Maximilian,McCabe, Stephanie R.,Wipf, Peter
supporting information
p. 6760 - 6764
(2018/10/25)

Fluorine-containing sulfonyl compound as well as intermediate, preparation method and application thereof
The invention discloses a fluorine-containing sulfonyl compound as well as an intermediate, a preparation method and application thereof. The fluorine-containing sulfonyl compound disclosed by the invention comprises positive ions and negative ions, wherein the positive ions are shown as the formula I. The fluorine-containing sulfonyl compound can react with substrates to effectively synthetize the fluorine-containing sulfonyl compound; the toxicity is low; the preparation is simple; the use is convenient; the fluorine-containing sulfonyl compound is in a solid stable state at normal temperature. In addition, the substrate applicability of the compound is extremely wide, and a phenol compound and an amine compound can be included; the fluorine-containing sulfonyl compound is a unique solidformation reagent capable of realizing the chemical conversion at present, so that important academic and application values are realized. The formula I is shown in the description.
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Paragraph 0402; 0403; 0404; 0405; 0406

(2018/05/24)

2-(Phenylseleno)ethanesulfon-amide as a novel protecting group for aniline that can be deprotected by a radical reaction
Anilines were protected as 2-(phenylseleno)ethanesulfonanilide (SeES anilide) via sulfonylation by 2-chlorosulfonyl chloride followed by the conjugate addition of benzeneselenol. The SeES anilide was deprotected by radical reduction using tributyltin hydride in the presence of AIBN. The corresponding anilines were obtained in high yields when the hydride and AIBN were added to the system slowly. Since the radical reaction proceeds under neutral conditions, chemoselective deprotection of the SeES group was accomplished. The SeES anilide was stable under various conditions, including some severe conditions.
Kihara, Nobuhiro,Mitsuhashi, Yuji,Sato, Makoto,Hirose, Shun-Ichi,Goudo, Erika,Uzawa, Yoshinori,Shirai, Natsumi,Hamamoto, Sari,Iwasaki, Ryo,Fujioka, Akane
supporting information
p. 2563 - 2566
(2016/06/06)

Pushing the Limits of Neutral Organic Electron Donors: A Tetra(iminophosphorano)-Substituted Bispyridinylidene
A new ground-state organic electron donor has been prepared that features four strongly π-donating iminophosphorano substituents on a bispyridinylidene skeleton. Cyclic voltammetry reveals a record redox potential of ?1.70 V vs. saturated calomel electrode (SCE) for the couple involving the neutral organic donor and its dication. This highly reducing organic compound can be isolated (44 %) or more conveniently generated in situ by a deprotonation reaction involving its readily prepared pyridinium ion precursor. This donor is able to reduce a variety of aryl halides, and, owing to its redox potential, was found to be the first organic donor to be effective in the thermally induced reductive S N bond cleavage of N,N-dialkylsulfonamides, and reductive hydrodecyanation of malonitriles.
Hanson, Samuel S.,Doni, Eswararao,Traboulsee, Kyle T.,Coulthard, Graeme,Murphy, John A.,Dyker, C. Adam
supporting information
p. 11236 - 11239
(2016/07/06)

Synthesis and biological evaluation of 1-(isoxazol-5-ylmethylaminoethyl)-4- phenyl tetrahydropyridine and piperidine derivatives as potent T-type calcium channel blockers with antinociceptive effect in a neuropathic pain model
New tetrahydropyridinyl and piperidinyl ethylamine derivatives were designed with hypothetical mapping on pharmacophore model generated from ligand-based virtual screening. The designed compounds were synthesized, and their inhibitory activities on T-type calcium channel were assayed using FDSS and patch-clamp assay. Among them, compounds 7b and 10b showed potent T-type calcium current blocking activity against Cav3.1 (α 1G) and Cav3.2 (α1H) channel simultaneously. With hERG and pharmacokinetics studies, compounds 7b and 10b were evaluated for the antinociceptive effect on rat model of neuropathic pain. They were significantly effective in decreasing the pain responses to mechanical and cold allodynia induced by spinal nerve ligation. These results suggest that modulation of α1G and α1H subtype T-type calcium channels may provide a promising approach for the treatment of neuropathic pain.
Lee, Ju-Hyeon,Seo, Seon Hee,Lim, Eun Jeong,Cho, Nam-Chul,Nam, Ghilsoo,Kang, Soon Bang,Pae, Ae Nim,Jeong, Nakcheol,Keum, Gyochang
p. 246 - 257
(2014/02/14)

Metal-free reductive cleavage of C-N and S-N bonds by photoactivated electron transfer from a neutral organic donor
A photoactivated neutral organic super electron donor cleaves challenging arenesulfonamides derived from dialkylamines at room temperature. It also cleaves a)ArC-NR and b)ArN-C bonds. This study also highlights the assistance given to these cleavage reactions by the groups attached to N in (a) and to C in (b), by lowering LUMO energies and by stabilizing the products of fragmentation. Radical fragmentations: Electron transfer from the photoactivated neutral electron donor 1 delivers high yields of S-N and C-N cleavage products for a range of nitrogen-containing species. These reactions proceed at room temperature and under mild reaction conditions in the absence of any metal reagents. DMF=N,N-dimethylformamide, Ts=4-toluenesulfonyl.
O'Sullivan, Steven,Doni, Eswararao,Tuttle, Tell,Murphy, John A.
supporting information
p. 474 - 478
(2014/01/23)

Visible-light photo-catalytic C-C bond cleavages: Preparations of N,N-dialkylformamides from 1,2-vicinal diamines
A range of 1,2-vicinal diamines were smoothly converted into N,N-dialkylformamides under the synergistic actions of Ru(bpy) 3Cl2 photo-catalyst, 45 W household lighting bulb, and Cs2CO3 basic additive under very mild reaction conditions. The process involves visible light-enabled photo-catalytic cleavage of C-C bond as the strategic event.
Zhao, Yaohong,Cai, Shunyou,Li, Jing,Wang, David Zhigang
supporting information
p. 8129 - 8131
(2013/08/28)

Reductions of challenging organic substrates by a nickel complex of a noninnocent crown carbene ligand
The first crown-tetracarbene complex of Ni(II) has been prepared, and its crystal structure determined. The complex can be reduced by Na/Hg, with an uptake of two electrons. The reduced complex reductively cleaves arenesulfonamides, including those derived from secondary aliphatic amines, and effects Birch reduction of anthracenes as well as reductive cleavage of stilbene oxides. Computational studies show that the orbital that receives electrons upon reduction of the complex 2 is predominantly based on the crown carbene ligand and also that the HOMO of the parent complex 2 is based on the ligand.
Findlay, Neil J.,Park, Stuart R.,Schoenebeck, Franziska,Cahard, Elise,Zhou, Sheng-Ze,Berlouis, Leonard E. A.,Spicer, Mark D.,Tuttle, Tell,Murphy, John A.
supporting information; experimental part
p. 15462 - 15464
(2011/02/22)

Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities
A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in elevated blood glucose in a murine model of type II diabetes.
Tang, Haifeng,Yan, Yan,Feng, Zhe,De Jesus, Reynalda K.,Yang, Lihu,Levorse, Dorothy A.,Owens, Karen A.,Akiyama, Taro E.,Bergeron, Raynald,Castriota, Gino A.,Doebber, Thomas W.,Ellsworth, Kenneth P.,Lassman, Michael E.,Li, Cai,Wu, Margaret S.,Zhang, Bei B.,Chapman, Kevin T.,Mills, Sander G.,Berger, Joel P.,Pasternak, Alexander
scheme or table
p. 6088 - 6092
(2010/11/18)

PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
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Page/Page column 129; 130

(2008/06/13)

SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE
The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.
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Page/Page column 173

(2008/06/13)

1,2 DIAMIDO CYCLOALKYL SODIUM CHANNEL BLOCKERS
1,2 Diamido cycloalkyl compounds that are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidin-dione and aryl-link-aryl oxazolodine-dione compounds and a pharmaceutically acceptable carrier; and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as irritable bowel syndrome, Crohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar disease, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolodine-dione compounds, either alone, or in combination with one or more therapeutically active compounds, are described.
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Page 74

(2010/11/30)

Substituted amine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer 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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(2008/06/13)

Substituted alkylamine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer 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 61; 83

(2010/02/05)

Highly potent geminal bisphosphonates. From pamidronate disodium (Aredia) to zoledronic acid (Zometa)
Bisphosphonates (BPs) are pyrophosphate analogues in which the oxygen in P-O-P has been replaced by a carbon, resulting in a metabolically stable P-C-P structure. Pamidronate (1b, Novartis), a second-generation BP, was the starting point for extensive SAR studies. Small changes of the structure of pamidronate lead to marked improvements of the inhibition of osteoclastic resorption potency. Alendronate (1c, MSD), with an extra methylene group in the N-alkyl chain, and olpadronate (1h, Gador), the N,N-dimethyl analogue, are about 10 times more potent than pamidronate. Extending one of the N-methyl groups of olpadronate to a pentyl substituent leads to ibandronate (1k, Roche, Boehringer-Mannheim), which is the most potent close analogue of pamidronate. Even slightly better antiresorptive potency is achieved with derivatives having a phenyl group linked via a short aliphatic tether of three to four atoms to nitrogen, the second substituent being preferentially a methyl group (e.g., 4g, 4j, 5d, or 5r). The most potent BPs are found in the series containing a heteroaromatic moiety (with at least one nitrogen atom), which is linked via a single methylene group to the geminal bisphosphonate unit. Zoledronic acid (6i), the most potent derivative, has an ED50 of 0.07 mg/kg in the TPTX in vivo assay after sc administration. It not only shows by far the highest therapeutic ratio when comparing resorption inhibition with undesired inhibition of bone mineralization but also exhibits superior renal tolerability. Zoledronic acid (6i) has thus been selected for clinical development under the registered trade name Zometa. The results of the clinical trials indicate that low doses are both efficacious and safe for the treatment of tumor-induced hypercalcemia, Paget's disease of bone, osteolytic metastases, and postmenopausal osteoporosis.
Widler, Leo,Jaeggi, Knut A.,Glatt, Markus,Müller, Klaus,Bachmann, Rolf,Bisping, Michael,Born, Anne-Ruth,Cortesi, Reto,Guiglia, Gabriela,Jeker, Heidi,Klein, Rémy,Ramseier, Ueli,Schmid, Johann,Schreiber, Gerard,Seltenmeyer, Yves,Green, Jonathan R.
p. 3721 - 3738
(2007/10/03)

Catalysis using phosphine oxide and sulfoxide compounds
Phosphine oxide and sulfoxide compounds were used with transition metals, preferably palladium and nickel, to produce biaryls, arylthiols, arylphosphine oxides and arylamines via cross-coupling reactions with aryl halides and arylboronic acids, aryl Grignard reagents, thiols, phosphine oxides or amines.
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(2008/06/13)

Tandem radical and non-radical reactions mediated with thiols - A new method of cleavage of allylic amines
Thiyl radical promotes the isomerisation of allylic amines into enamines via two consecutive hydrogen atom abstraction steps, and the subsequent polar addition of the corresponding thiol to the enamine results in the cleavage of the C-N bond via a thioaminal intermediate: this reaction provides a mild, metal-free methodology for the deprotection of allylated primary and secondary amines.
Bertrand, Michele P.,Escoubet, Stephanie,Gastaldi, Stephane,Timokhin, Vitaliy I.
p. 216 - 217
(2007/10/03)

Catalysis using phosphine oxide compounds
Phosphine oxide compounds were used with transition metals, preferably palladium and nickel, to produce biaryls and arylamines via cross-coupling reactions with aryl halides and arylboronic acids, aryl Grignard reagents or amines.
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(2008/06/13)

3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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(2008/06/13)

Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors
Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.
Sakamuri, Sukumar,Enyedy, Istvan J,Kozikowski, Alan P,Zaman, Wahiduz A,Johnson, Kenneth M,Wang, Shaomeng
p. 495 - 500
(2007/10/03)

Superacid-catalyzed preparation of aryl-substituted piperidines via dicationic electrophiles
The electrophilic chemistry of 1,2,3,6-tetrahydropyridines has been studied in the Bronsted superacid, CF3SO3H (triflic acid). The 1,2,3,6-tetrahydropyridines react with arenes to give aryl-substituted piperidines. It is proposed tha
Klumpp, Douglas A.,Beauchamp, Philip S.,Sanchez Jr., Gregorio V.,Aguirre, Sharon,De Leon, Sarah
p. 5821 - 5823
(2007/10/03)

Catalysis using phosphine oxide compounds
Phosphine oxide compounds were used with transition metals, preferably palladium, to produce biaryls and arylamines via cross-coupling reactions with aryl halides and arylboronic acids or amines.
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(2008/06/13)

14-substituted marcfortines and derivatives useful as antiparasitic agents
There are disclosed 14α-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I). STR1
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(2008/06/13)

Dihydropyridine derivatives for treatment of benign prostatic hyperplasia.
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(2008/06/13)

Marcfortine/paraherquamide derivatives useful as antiparasitic agents
There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants. Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.
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(2008/06/13)

Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
This invention relates to compounds of Formula I STR1 which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
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(2008/06/13)

Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
This invention relates to compounds of Formula I STR1 which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.
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(2008/06/13)

Pharmaceutically-active phthalazine compounds
Compounds having the formula STR1 wherein R is 2-[1-oxo-(2H)-phthalazinyl], R1, R2, R3, R4, R5, R6, X, Y, m and n have the meanings shown in the description. The compounds of formula I are pharmaceutically active as anti-vasospastic, anti-aggregating, and anti-proliferative agents.
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(2008/06/13)

Preparation of substituted piperidines
Piperidines substituted in the 3- and/or 4-position are prepared by reacting a glutardialdehyde substituted in the 2- and/or 3-position with ammonia or a primary amine and hydrogen at elevated temperature and under superatmospheric pressure in the presence of a hydrogenation catalyst.
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(2008/06/13)

THE MILD AND SELECTIVE N-DEBENZYLATION OF TERTIARY ALKYLAMINES USING β-TRIMETHYLSILYLETHYL CHLOROFORMATE.
Benzyl groups are efficiently and selectively cleaved from tertiary alkylamines using β-trimethylsilylethyl chloroformate.This general method is compatible with a wide range of functionality because it does not require strong hydrolytic or acidic solvolytic conditions.
Campbell, Arthur L.,Pilipauskas, R. Allen,Khanna, Ish K.,Rhodes, R. Allen
p. 2331 - 2334
(2007/10/02)

Treatment of atherosclerosis with khellin-related furochromones
The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
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(2008/06/13)

Antiatherosclerotic furochromones
The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
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(2008/06/13)