- Synthesis and characterization of novel analogues of cefpodoxime proxetil
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The present work describes the origin, identification, synthesis, characterization and control of four novel analogues of cefpodoxime proxetil, which are ethyl, methyl, propyl and N-propyl analogues of cefpodoxime proxetil.
- Reddy, Peketi Rajesh,Musunuri, Sivanadh,Reddy, D. Ramasekhara,Chittala, V. Subrahmanyam,Murthy,Krishnamohan
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p. 1751 - 1755
(2020/07/30)
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- Regioselective synthesis of 2-O-acyl-3-O-(1-acyloxyalkyl) prodrugs of 5,6-isopropylidene-L-ascorbic acid
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An efficient regioselective synthesis of 2-O-acyl-3-O-(1-acyloxyalkyl) prodrugs of vitamin C 5,6-acetonide has been developed which does not involve tedious column chromatographic separation of the desired products from contaminants exhibiting very similar Rf values. Vitamin C 5,6-acetonide is first acylated with one equivalent of acyl halide in the presence of two equivalents of pyridine. The crude 2-O-acylated product is then alkylated with one equivalent of 1-acyloxyalkyl-1-iodide in the presence of one equivalent of triethylamine. The 2-O-acyl-3-O-(1-acyloxyalkyl) vitamin C 5,6-acetonides are obtained in moderate yields.
- Prybylski, John,Thiele, Nikki A.,Sloan, Kenneth B.
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supporting information
p. 1619 - 1621
(2018/03/27)
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- 3,3-DISUBSTITUTED-1-HYDROXYTRIAZ-1-ENE 2-OXIDES AND WOUND-HEALING COMPOSITIONS USING THEM
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Esters, carbonates and imides of 3,3-disubstituted-1-hydroxytriaz-1-ene 2-oxides of the formula I are disclosed. The compounds release nitric oxide (NO) under physiologic conditions, and pharmaceutical compositions containing them are useful to aid in wound healing.
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Paragraph 00122
(2015/08/03)
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- NO-RELEASING NONOATE (NITROGEN-BOUND) SULFONAMIDE-LINKED-COXIB ANTI-CANCER AGENTS
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The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide- linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).
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Paragraph 00155; 00156
(2014/02/15)
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- N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE
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The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
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Page/Page column 164
(2012/05/20)
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- GABA ANALOGS, COMPOSITIONS, AND METHODS FOR MANUFACTURING THEREOF
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The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.
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Page/Page column 15-16
(2009/10/22)
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- GABA ANALOGS, COMPOSITIONS AND METHODS FOR MANUFACTURING THEREOF
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The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.
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Page/Page column 6
(2008/12/05)
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- BENZIMIDAZOLE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
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The present invention relates to a compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has superior stability to acid and which is a prodrug of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole. This compound (1) shows a superior anti-ulcer activity, a gastric acid secretion-suppressive action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like in living organisms, (2) shows low toxicity, (3) shows superior stability to acid (which obviates the need to formulate an enteric-coated preparation, thereby lowering the cost, and reduces the size of preparation to facilitate swallowing for patients having difficulty in swallowing), (4) shows faster absorption than enteric-coated preparations (rapid expression of gastric acid secretion-suppressive action), and (5) is sustainable.
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- Studies on nonpeptide angiotensin II receptor antagonists. II. Synthesis and biological evaluation of 5H-pyrazolo[1,5-b][1,2,4]triazole derivatives with a C-linked oxygen functional group at the 6-position
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2,7-Diethyl-5H-pyrazolo[1,5-b][1,2,4]triazole derivatives were synthesized and evaluated for activity as angiotensin II receptor antagonists. Replacement of the C-6 hydrogen with C-linked oxygen functional groups led to derivatives with increased in vitro
- Okazaki, Toshio,Suga, Akira,Watanabe, Toshihiro,Kikuchi, Kazumi,Kurihara, Hiroyuki,Shibasaki, Masayuki,Fujimori, Akira,Inagaki, Osamu,Yanagisawa, Isao
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p. 287 - 293
(2007/10/03)
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- Studies on nonpeptide angiotensin II receptor antagonists. IV. Synthesis and biological evaluation of 4-acrylamide-1H-imidazole derivatives
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A novel series of nonpeptide angiotensin II antagonists containing the acrylamide group at the 4-position of the imidazole ring was synthesized and their antagonistic activity was examined by functional assay in rabbit aorta. The acrylamide group was selected as a large lipophilic surrogate for the chloro group of EXP3174. A structure-activity relationship study of the acrylamide moiety has shown that substitution at the 4-position with the N- methyl-3,3-dimethylacrylamide group resulted in the optimal compound, 2- butyl-4-[(3,3-dimethylacryloyl)methyl-amino]-1-[[2'-(1H-tetrazol-5- yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic acid (1), which was superior to EXP3174 in vitro. Since 1 showed only poor activity against angiotensin II-induced pressor response in rats after oral administration, the carboxylic acid function of 1 was converted into prodrug esters (13). Among these, the 1-[(ethoxycarbonyl)oxy]ethyl ester (13a) showed the most potent and longest-lasting activity when given orally to rats. When administered orally to conscious furosemide-treated dogs, 13a showed an approximately 3-fold increased hypotensive activity in comparison with DuP 753. These data suggest that 13a may be an useful agent for the treatment of angiotensin II-dependent diseases, such as hypertension.
- Okazaki, Toshio,Watanabe, Toshihiro,Kikuchi, Kazumi,Suga, Akira,Shibasaki, Masayuki,Fujimori, Akira,Inagaki, Osamu,Yanagisawa, Isao
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p. 973 - 981
(2007/10/03)
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- Synthesis of iodoalkylacylates and their use in the preparation of S-alkyl phosphorothiolates
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Synthesis of iodoalkylacylates 3a-f and use of 3c in the preparation of an oligonucleoside phosphorothiate prodrug analog 5 is described.
- Iyer,Yu,Ho,Agrawal
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p. 2739 - 2749
(2007/10/02)
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- Cephalosporin analogs for oral use
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7β-(2-Cyano-aliphatic acylamino)-7α-methoxy-3-heterocyclic thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acids and salts or pharmacologically acceptable esters generically represented by the following formula are potent antibacterials and esters are prospective oral drugs: STR1 (wherein A is a lower alkyl, lower alkenyl or lower alkynyl group; B is a hydrogen atom, salt forming atom, salt forming group or physiologically hydrolyzable ester group; and Het is a heterocyclic group).
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