- Preparation method of high-purity cefotiam hexetil dihydrochloride
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The invention discloses a preparation method of cefotiam hexetil dihydrochloride. The method comprises the steps that cefotiam hydrochloride is used as a raw material for synthesizing cefotiam alkali metal salt; the cefotiam alkali metal salt and 1-iodoet
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Paragraph 0045; 0046; 0047
(2017/08/29)
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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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- 2-ARYLMETHYLAZETIDINE-CARBAPENEM-3-CARBOXYLIC ACID ESTER DERIVATIVE OR ITS SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides a 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives or their pharmaceutically acceptable salts show high oral absorption rate, and thus can be orally administered. The active metabolites thereof have a broad spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against methicillin-resistant Staphylococcus aurus (MRSA) and quinolone-resistant strains (QRS). In particular, the acid addition salts of the 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives are obtained in crystalline forms having excellent stability.
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Page/Page column 18
(2009/06/27)
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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 7
(2008/12/05)
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- METHOD FOR PRODUCTION OF CANDESARTAN
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The invention relates to novel methods for the production of Candesartan, or a protected form of Candesartan, a Candesartan salt or ester, compounds of application in said method, methods for production thereof, use thereof in said method, a novel polymorph of Candesartan cilexetil, a method for production and use thereof for production of a medicament.
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Page/Page column 24-25
(2010/11/08)
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- NOVEL PHENYLALANINE DERIVATIVE
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The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.
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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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- Prodrugs of CL316243: A selective β3-adrenergic receptor agonist for treating obesity and diabetes
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CL316243 is a highly selective and potent β3-adrenergic receptor agonist, and has been shown in rodent models to be an effective agent for treating obesity and Type II diabetes. To improve the oral absorption and pharmacokinetic profiles of CL316243, a number of prodrugs have been synthesized and evaluated. Several ester-type prodrugs show significant improvements in oral bioavailability in both rodent and primate models.
- Sum,Gilbert,Venkatesan,Lim,Wong,O'Dell,Francisco,Chen,Grosu,Baker,Ellingboe,Malamas,Gunawan,Primeau,Largis,Steiner
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p. 1921 - 1926
(2007/10/03)
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- Cephalosporin ester derivatives
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A compound of the formula: STR1 wherein R1 is a hydrogen atom or a lower alkyl group; R2 is an unsubstituted or lower alkyl-substituted alicyclic alkyl group of 3 to 12 carbon atoms or a C3-6 alicyclic alkyl-substituted lower alkyl group or a pharmaceutically acceptable salt thereof, processes for preparing the same, a pharmaceutical composition thereof are provided. The compound has an improved absorbability and can be orally applied as antibiotics.
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- Antibacterial solid composition for oral administration
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This invention relates to an antibacterial solid composition for oral administration which comprises a lipid soluble cephalosporin compound and a cyclodextrin. The said composition provides much increased in vivo absorbability of a non-ester form of the cephalosporin compound. This composition is useful for prevention and treatment of bacterial infections.
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