- HETEROARYL DERIVATIVES AS SEPIAPTERIN REDUCTASE INHIBITORS
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Inhibitors of sepiapterin reductase of formula (I) or (I'), wherein the substituents are defined as in the claims, and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.
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Paragraph 00441-00443
(2017/05/31)
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- Method for preparing 2-formyl-3-ethyl oxopropionate
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The invention relates to a method for preparing 2-formyl-3-ethyl oxopropionate. The method comprises the steps of subsequently adding ethanol, potassium carbonate, ethyl formate and NaH into vinyl ethyl ether and trichloro-acetyl chloride, which serve as starting raw materials, and carrying out multistep reactions, thereby obtaining 2-formyl-3-ethyl oxopropionate. The obtained final product has the purity of 99.7% and the yield of 45%. The method is readily available in raw materials, mild in reaction conditions and low in cost and is applicable to large-scale production in factories.
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Paragraph 0007; 0022; 0023
(2017/09/01)
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- Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents
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To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity. Many of the target compounds showed good inhibitory activity against Candida albicans and Cryptococcus neoformans. In particular, the isoxazole nuclei were more suited for improving the activity against Aspergillus spp. Among these compounds, 2-F substituted analogues 23g and 23h displayed the most remarkable in vitro activity against Candida spp., C. neoformans, A. fumigatus and fluconazole-resistant C.alb. strains, which is superior or comparable to the activity of the reference drugs fluconazole and voriconazole. Notably, the compounds 23g and 23h exhibited low inhibition profiles for various isoforms of human cytochrome P450 and excellent blood plasma stability.
- Zhao, Shizhen,Zhang, Xiangqian,Wei, Peng,Su, Xin,Zhao, Liyu,Wu, Mengya,Hao, Chenzhou,Liu, Chunchi,Zhao, Dongmei,Cheng, Maosheng
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- BMP INHIBITORS AND METHODS OF USE THEREOF
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The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
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Page/Page column 67
(2014/10/15)
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- Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against mycobacterium tuberculosis
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DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clinical value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochemical studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis.
- Hameed P, Shahul,Patil, Vikas,Solapure, Suresh,Sharma, Umender,Madhavapeddi, Prashanti,Raichurkar, Anandkumar,Chinnapattu, Murugan,Manjrekar, Praveena,Shanbhag, Gajanan,Puttur, Jayashree,Shinde, Vikas,Menasinakai, Sreenivasaiah,Rudrapatana, Suresh,Achar, Vijayashree,Awasthy, Disha,Nandishaiah, Radha,Humnabadkar, Vaishali,Ghosh, Anirban,Narayan, Chandan,Ramya,Kaur, Parvinder,Sharma, Sreevalli,Werngren, Jim,Hoffner, Sven,Panduga, Vijender,Kumar, C. N. Naveen,Reddy, Jitendar,Kumar Kn, Mahesh,Ganguly, Samit,Bharath, Sowmya,Bheemarao, Ugarkar,Mukherjee, Kakoli,Arora, Uma,Gaonkar, Sheshagiri,Coulson, Michelle,Waterson, David,Sambandamurthy, Vasan K.,De Sousa, Sunita M.
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supporting information
p. 4889 - 4905
(2014/07/07)
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- Bu3SnH-mediated radical cyclisation onto azoles
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Alkyl radicals have been cyclised onto pyrroles, imidazoles and pyrazoles, and acyl radicals cyclised onto pyrroles, using Bu3SnH-, (TMS)3SiH- and Bu3GeH-mediated aromatic homolytic substitution for the synthesis of bicyclic N-heterocycles. The reactions yield intermediate π-radicals that lose hydrogen in the?rearomatisation step of the aromatic homolytic substitution. Mechanistic studies of these rearomatisation steps indicate aromatic homolytic substitution in which the initiator or breakdown products from the inhibitor are responsible for the H-abstraction step.
- Allin, Steven M.,Barton, William R.S.,Russell Bowman,Bridge (née Mann), Emma,Elsegood, Mark R.J.,McInally, Tom,McKee, Vickie
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p. 7745 - 7758
(2008/12/21)
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- PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS
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Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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Page/Page column 20
(2009/01/20)
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- PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS
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Disclosed is a synthesis suitable for large scale manufacture of an A2A- adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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Page/Page column 17-18
(2008/06/13)
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- Adamantyl-pyrazole carboxamides as inhibitors of 11B-hydroxysteroid dehydrogenase
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
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Page/Page column 30-31
(2008/06/13)
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- FUSED THIAZOLE DERIVATIVES HAVING AFFINITY FOR THE HISTAMINE H3 RECEPTOR
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The present invention relates to novel fused thiazole derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
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Page/Page column 32
(2008/06/13)
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- Herbicide compositions
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A herbicidal composition which comprises i) an isoxazoline derivative represented by the following general formula (I) or its salt and ii) at least one compound selected from the Group A: Formula (I) wherein R1, R2, R3, R4, R5 and R6 are defined in the specification.
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Page/Page column 31-32
(2010/02/14)
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- ISOXAZOLINE DERIVATIVE AND HERBICIDE COMPRISING THE SAME AS ACTIVE INGREDIENT
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An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; ???R3, R4, R5 and R6 are each a hydrogen atom; ???Y is an optionally substituted 5- to 6-membered aromatic heterocyclic group or fused aromatic heterocyclic group having a hetero atom selected from a nitrogen atom, a oxygen atom and a sulfur atom; and ???n is an integer of 0 to 2. The isoxazoline derivative has an excellent herbicidal effect and an excellent selectivity between crop and weed.
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Page/Page column 196
(2010/02/07)
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- A Facile Synthesis of Polyfunctionally Substituted Pyridines from Ethoxycarbonylmalonaldehyde
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A facile access to 2,3-disubstituted-5-ethoxycarbonylpyridines (50-66percent yields), derivatives of biologically and medicinally important nicotinic acid, is explored.The method involves the reaction of ethoxycarbonylmalonaldehyde with tosyl chloride and then with β-amino-α,β-unsaturated esters, ketones, or nitriles in the presence of pyridine.
- Torii, Sigeru,Inokuchi, Tsutomu,Kubota, Minoru
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p. 400 - 402
(2007/10/02)
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- ISOLATION, STRUCTURE AND SYNTHESIS OF 4-HYDROXYISOXAZOLE (TRIUMFEROL), A SEED GERMINATION INHIBITOR FROM AN AFRICAN PLANT
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The isolation, characterization and an efficient synthesis of 4-hydroxyisoxazole 1, a plant growth regulator isolated from an African plant is reported.It is a new compound, which despite the simple structure, had eluded synthesis.
- Kusumi, Takenori,Chang, Conway C.,Wheeler, Margaret,Kubo, Isao,Nakanishi, Koji,Naoki, Hideo
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p. 3451 - 3454
(2007/10/02)
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