- PROCESS FOR PURIFYING (METH)ACRYLIC ACID
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A process for producing a grade of (meth)acrylic acid having residual formaldehyde levels of under 100 parts per million.
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Page/Page column 7-8
(2014/10/03)
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- Synthesis and biological activity of novel L-amino acid based analgesic compounds
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Synthesis and analgesic activity studies of a series of L-amino acid based compounds were described. These compounds were designed as potential N-type Calcium Channel Blockers and their structures were confirmed by 1H NMR and ESI-MS spectra. Some of the compounds exhibited significant analgesic activity in Mouse Hot-Plate tests. According to the data of pharmacological experiments, we carried out preliminary structure-activity studies and the results indicated that this kind of compounds was useful for the development of new analgesic drugs.
- Pan, Junzhu,Wang, Qianqian,He, Gu,Ouyang, Liang,Guo, Li
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scheme or table
p. 359 - 364
(2011/10/31)
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- EFFICIENT SYNTHESIS OF CHELATORS FOR NUCLEAR IMAGING AND RADIOTHERAPY: COMPOSITIONS AND APPLICATIONS
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Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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Page/Page column 95-96
(2008/06/13)
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- HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITION FOR INHIBITING LIPID ACCUMULATION CONTAINING SAME
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The present invention relates to a novel heterocyclic carboxylic acid derivative, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for inhibiting the accumulation of lipids in the body.
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Page/Page column 54
(2008/12/04)
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- NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESS FOR THEIR PREPARATION
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The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: (I) wherein Y is -S(O)m, -CH2-, CHF, or -CF2; m is 0, 1, or 2; X is a bond, C1-C5 alkyl (e.g., -CH2-), or -C(=0)-; the dotted line [----] in the carbocyclic ring represents an optional double bond; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted heteroarylalkyl, CN, -COOR3, CONR3R4, -OR3, -NR3R4, or NR3COR3; R2 is hydrogen, cyano, COOH, or an isostere of a carboxylic acid (such as SO3H, CONOH, B(OH)2, PO3R3R4, SO2NR3R4, tetrazole, -COOR3, -CONR3R4, NR3COR4, or -COOCOR3).
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Page/Page column 45
(2008/06/13)
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- NEW ADAMANTANE DERIVATIVES AS DIPEPTIDYL, PEPTIDASE IV INHIBITORS, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula (A): wherein R1, R2, Y, and n are as defined herein, pharmaceutical compositions containing the same, processes for their preparation, and methods for treating disorders mediated by DPP-IV inhibition, such as diabetes, especially Type II diabetes, with them.
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Page/Page column 30
(2008/06/13)
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- NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS; PROCESSES FOR THEIR PREPARATION AND COMPOSITIONS THEREOF
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The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors or general formula (1) useful for treating diabetes, non-insulin dependent diabetes mellitus, impaired glucose tolerance, inflammatory bowel disease, ulcerative colitis,Chron’s disease, obesity, and metabolic syndrome.
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Page/Page column 37
(2008/06/13)
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- Inhibitors of α4β1 mediated cell adhesion
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The present invention relates to compound of formula (I), that are potent inhibitors of α4β1mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing α4β1adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.
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Page/Page column 26
(2010/02/05)
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- Azafulvenium methides: New extended dipolar systems
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The transient 8π 1,7-dipolar azafulvenium methides 5 and 8 undergo sigmatropic [1,8] H shifts and the acyl derivatives 12 electrocyclise to give novel pyrrolooxazines 13; the related diazafulvenium methide 15 can be intercepted in 8π + 2π cycloadditions with silylated acetylenes.
- Sutcliffe, Oliver B.,Storr, Richard C.,Gilchrist, Thomas L.,Rafferty, Paul,Crew, Andrew P. A.
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p. 675 - 676
(2007/10/03)
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- 14-substituted marcfortines and derivatives useful as antiparasitic agents
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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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- Marcfortine/paraherquamide derivatives useful as antiparasitic agents
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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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- Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
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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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- Preparations of Optically Active Homocysteine and Homocystine by Asymmetric Transformation of (RS)-1,3-Thiazane-4-carboxylic Acid
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DL-Homocysteine from (RS)-homocysteine thiolactone hydrochloride was subjected to reaction with formaldehyde in acetic acid to give (RS)-1,3-thiazane-4-carboxylic acid monohydrate .An asymmetric transformation of (RS)-THA*H2O was achieved via salt formation with optically active tartaric acid in the presence of salicylaldehyde in acetic acid.The (R)- and (S)-THA obtained, respectively, from the salt of (R)-THA with (2R,3R)-tartaric acid and its enantiomeric salt were treated with hydroxylamine hydrochloride to give D- and L-Hcy of 100percent optical purity, respectively, in 50percent yield from (RS)-HTL*HCl.Oxidation of D- and L-Hcy with hydrogen peroxide gave D- and L-homocystine, respectively, in 47percent yield.
- Miyazaki, Hideya,Ohta, Atsushi,Kawakatsu, Nobuyuki,Waki, Yukitaka,Gogun, Yasuhiro,et al.
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p. 536 - 540
(2007/10/02)
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- Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
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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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- Optical Resolution by Replacing Crystallization of (RS)-4-Thiazolidinecarboxylic Acid with L-Amino Acids as Cosolute
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The optical resolution by replacing crystallization of (RS)-4-thiazolidinecarboxylic acid was carried out with coexisting eight L-amino acids and the effect of the latter was examined.L-Isoleucine and L-cysteine as the cosolute led to preferential crystallization of (R)-THC from an aqueous solution of (RS)-THC, whereas the other L-amino acids gave (S)-THC.L-Cys, L-threonine, L-4-hydroxyproline , and L-serine as the cosolute seemed to give better selectivity for crystallization of one enantiomer than L-Ile, L-valine, L-proline, and L-alanine.The optical resolution with L-Hyp was successfully achieved and suggested a possibility of successive optical resolution to give both (R)- and (S)-THC.
- Shiraiwa, Tadashi,Yamauchi, Masahiro,Tatsumi, Takeshi,Kurokawa, Hidemoto
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p. 267 - 273
(2007/10/02)
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- Asymmetric Transformation of (RS)-Cysteine via Formation of (RS)-4-Thiazolidinecarboxylic Acids
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Either (R)- or (S)-cysteine ((R)- or (S)-Cys) was efficiently obtained from (RS)-Cys by the asymmetric transformation via formation of (RS)-thiazolidinecarboxylic acid ((RS)-THC) or (RS)-2,2-dimethyl-4-thiazolidinecarboxylic acid ((RS)-DMZ) and by using (2R,3R)- or (2S,3S)-tartaric acid ((R)- or (S)-TA), as a resolving agent, in acetic acid.The asymmetric transformation was carried out by combination of crystallization of less soluble salt of (S)-THC or -DMT with (R)-TA (or salt of (R)-THC or -DMT with (S)-TA) and epimerization of soluble diastereomeric salt.The (R)- and (S)-THCs from the less soluble salts gave approximately optically pure (R)- and (S)-Cys's, respectively, in 64percent yield.The asymmetric transformation via formation of (RS)-DMT was more succeefully achieved by adding 0.1 molar equivalent of salicylaldehyde; that is, hydrolysis of the obtained less soluble salt gave optically pure (R)- and (S)-Cys's, respectively, in 80percent yield based on the (RS)-Cys used as the starting material.
- Shiraiwa, Tadashi,Kataoka, Kazuo,Sakata, Shinji,Kurokawa, Hidemoto
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p. 109 - 113
(2007/10/02)
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- A Dipolar Cycloaddition Approach to Pyrroloindoles Using N--Substituted Indoles
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The 1,3-dipolar cyloaddition of a number of N--substituted indoles with several dipolarophiles has been investigated.The reaction requires the use of an equivalent amount of silver fluoride and provides a direct and efficient synthesis of the pyrroloindole ring system.The structures of the cycloadducts were established by high-field NMR spectroscopy as well as by several X-ray crystal structures.The cycloaddition reactions show all the characteristics of a concerted reaction, including complete stereospecificity and regioselectivity.The results are consistent with a mechanism that involves the intermediacy of an azomethine ylide.Formation of the dipole is rationalized by assuming that silver ion behaves as a very specific Lewis acid that attacks the indole ring to give a silver bonded carbonium ion.This is followed by a rapid desilylation reaction to give the azomethine ylide.After the cycloaddition step, the resulting silver-bonded intermediate undergoes consecutive loss of silver and a hydrogen to give the observed product.Attempts to extend the cycloaddition methodology to N--substituted enamines and pyrroles are also described.
- Padwa, Albert,Fryxell, Glen E.,Gasdaska, John R.,Venkatramanan, M. K.,Wong, George S. K.
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p. 644 - 653
(2007/10/02)
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- Asymmetric Transformation of DL-4-Thiazolidinecarboxylic Acid
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A mixture of DL-4-thiazolidinecarboxylic acid (DL-THC), (+)- or (-)-tartaric acid ((+)- or (-)-TA), and salicylaldehyde in acetic acid was stirred at 80 deg C to give a salt composed of equimolar amounts of L-THC and (-)-TA or that of D-THC and (+)-TA.D- and L-THC with optical purity of 97-99percent were obtained from these salts in 68-78percent yield.
- Shiraiwa, Tadashi,Kataoka, Kazuo,Kurokawa, Hidemoto
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p. 2041 - 2042
(2007/10/02)
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- Optical Resolution by Preferential Crystallization of DL-Thiazolidine-4-carboxylic Acid
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Infrared spectrum, solubility, and ternary solubility diagram indicated that DL-thiazolidine-4-carboxylic acid (DL-THC) is a conglomerate at room temperature.The free energy of critical nucleation in supersaturated solutions for the crystallization of D- and L-THC was examined to resolve DL-THC efficiently by preferential crystallization.Successive preferential crystallization of DL-THC was experimented at 20 deg C for an aqueous racemic solution with a supersaturation of 150percent, and D- and L-THC with optical purity 96-100percent were obtained in the range of resolution of 58-76percent.The optical resolution was more succesfully done in 1 mol dm-3 aqueous glycine to give D- and L-THC with optical purity of 93-99percent in the degree of resolution of 77-87percent.Recrystallization of D- and L-THC obtained with a succeeding treatment with hydroxylamine hydrochloride gave D- and L-cysteine with 100percent optical purity.
- Shiraiwa, Tadashi,Sado, Yujin,Komure, Masamitsu,Kurokawa, Hidemoto
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p. 3277 - 3284
(2007/10/02)
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- Thiolic derivatives of erythromycin having therapeutic activity, and pharmaceutical compositions containing them
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The thiolic salts of erythromycin and of the propionic ester of erythromycin with thenoyl alpha-mercaptopropionylglycine find therapeutical use in the cases in which erythromycin or its propionic ester are used and are generally endowed with very low toxicity and high hematic levels.
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- Treatment of atherosclerosis with khellin-related furochromones
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The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
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- Antiatherosclerotic furochromones
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The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
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