- MLKL INHIBITORS
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Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
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Paragraph 0997-0999
(2018/09/26)
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- PROCEDURE FOR THE PREPARATION OF 2-CYANOIMINO-1,3-THIAZOLIDINE
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The disclosure provides for methods for preparing 2-cyanoimino-l,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-l,3-thiazolidine.
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Paragraph 0082; 0088; 0091; 0092
(2017/04/11)
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- An antibiotic anticancer activity method for the preparation of compounds
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The invention discloses a preparation method of an antibacterial anti-cancer active compound. The preparation method comprises the following steps: under cooling in an ice bath, enabling a compound HRB-1365-0, a compound HRB-1365-1 and water to react at a
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Paragraph 0051; 0052; 0061
(2018/07/10)
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- An antibiotic anticancer active compound
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The invention discloses an anti-bacterial and anti-cancer active compound. The anti-bacterial and anti-cancer active compound or an addition product thereof is shown in the specification, wherein substituent groups of R1, R2, R3 and R4 are selected from a hydroxyl, an amino group, a nitryl, a halogen atom, a hydrogen atom, a C1-6 alkyl, a C2-6 alkenyl, a C6-10 aryl, a C1-6 alkyl acylamino group or a C1-6 alkoxy carbonyl. A novel compound is prepared by a hydrochloride salt, has an anti-bacterial effect and significant anti-cancer activity, and has good clinical application values.
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Paragraph 0042-0046
(2017/04/28)
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- PROCESS FOR PREPARING CYANIMINO-1,3-THIAZOLIDINES
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The present invention relates to a process for preparing cyanimino-1,3-thiazolidines, which are important building blocks for the preparation of crop protection active ingredients and pharmaceuticals, by the following scheme: where A is an alkali metal an
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Page/Page column 5
(2009/04/25)
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- A PROCESS FOR THE PREPARATION OF 2-CYANOIMINO-1,3-THIAZOLIDINE
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The present invention relates to a process for the preparation of substantially pure 2-cyanoimino-1, 3-thiazolidine of Formula (I) by cyclization of dimethyl N-cyanoiminodithiocarbonate with 2-aminoethanethiol or the salt thereof in the presence of an alk
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Page/Page column 14-15
(2009/10/22)
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- PROCESS FOR PRODUCING 2-CYANOIMINO-1,3-THIAZOLIDINE
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A method of obtaining a high purity 2-cyanoimino-1,3-thiazolidine, at a high yield, by cyclization reaction of dimethyl N-cyanoiminodithiocarbonate ester with 2-aminoethane thiol or the salt thereof in the presence of an alkali metal hydroxide is disclose
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- Azido-neonicotinoids as candidate photoaffinity probes for insect nicotinic acetylcholine receptors [1]
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The neonicotinoids are the most successful chemical class of insecticides reaching sales of more than 630 Mio $ in 2001, mainly due to the excellent market performance of imidacloprid and thiamethoxam. The insect nicotinic acetylcholine receptors (nAChRs) are the targets for these compounds, which are highly effective against a variety of sucking and chewing insects. Compared with the other neonicotinoid sales products, thiamethoxam binds in a different way, possibly to a different site of nAChRs in aphids. To gain further insight into the different modes of binding, a research program applying the photoaffinity labeling technique was started. A series of novel candidate photoaffinity probes containing a 5-azido-6-chloropyridin-3-ylmethyl group were prepared from 5-azido-6-chloropyridin-3-ylmethyl chloride, which was obtained in three steps from 6-chloropyridin-3-ylmethyl chloride. These probes showed good to excellent contact/feeding and systemic activity against Myzus persicae, however, they were at least 4- to 16-fold less effective against Aphis craccivora, Nilaparvata lugens, Spodoptera littoralis, and Diabrotica balteata than the neonicotinoid sales products. In general, the introduction of an azide group at C(5) of the 6-chloropyridin-3-ylmethyl substituent resulted in reduced potency as well as in a narrower pest spectrum. In competition binding assays with [3H]imidacloprid, analogues of imidacloprid, clothianidin, thiacloprid and thiamethoxam containing a 5-azido-6-chloropyridin- 3-ylmethyl group showed high displacing potency with nAChRs from Aphis and Myzus (Ki values: 2 to 27 nM) suggesting that these compounds are valuable candidate photoaffinity probes. Taking into account the biological screening activity as well as the receptor binding potency, 1-(5-azido-6- chloropyridin-3-ylmethyl)-2-nitroimino-imidazolidine N-(5-azido-6-chloropyridin- 3-ylmethyl)-N′-methyl-N″-nitroguanidine and 3-(5-azido-6- chloropyridin-3-ylmethyl)-2-cyanoimino-thiazolidine were identified as the preferred candidate neonicotinoid photoaffinity probes to study the imidacloprid binding site.
- Maienfisch, Peter,Haettenschwiler, Joerg,Rindlisbacher, Alfred,Decock, Arnaud,Wellmann, Henning,Kayser, Hartmut
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p. 710 - 714
(2007/10/03)
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- Method of production of 2-cyanoimino-1, 3-thiazolidine
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A method for producing high purity 2-cyanoimino-1,3-thiazolidine comprising the steps of: reacting an alkali metal cyanide compound, an alkali metal hydroxide, a lower alcohol and chlorine in an aqueous solution to form an carboimidic acid ester solution, then adding an organic solvent thereto, followed by adding a cyanamide solution to form an N-cyanocarbonimidic acid ester, and further extracting the resultant ester with an organic solvent extracting solution, followed by washing with an aqueous solution of a reducing agent solution to obtain a high purity, stable N-cyanocarbonimidic acid ester as a first step; and reacting the N-cyanocarbonimidic acid ester obtained in the first step with 2-aminoethanethiol to be cyclicized as a second step to thereby obtain a 2-cyanoimino-1,3-thiazolidine.
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- Process for the production of 2-cyanoiminothiazolidine
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A process for the production of 2-cyanoiminothiazolidine by reaction of 2-aminoethanethiol (cysteamine) with a dialkyl-N-cyanoimidocarbonate.
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- Reaction of 3-aralkylsulfonyl-2-(N-cyanoimino)-thiazolidines with oxygen nucleophiles
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3-Aralkylsulfonyl-2-(N-cyanoimino)thiazolidines react with oxygen nucleophiles, such as sodium alkoxides and carboxylates, at the 3-sulfonyl group to give 3-alkyl- and 3-acyl-2-(N-cyanoimino)thiazolidines, respectively.
- Tanaka, Tetsuaki,Nakamoto, Yumi,Maekawa, Kaori,Watanabe, Mayumi,Nishihara, Chihiro,Iwata, Chuzo,Uchida, Shuji
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p. 265 - 272
(2007/10/02)
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- Process for the preparation of cyanoimino-1,3-thiazolidines
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X is an acid radical, and A is a metal ion or an equivalent ammonium ion.
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- Anomalous One-pot Transformation of 3-Dimethoxymethyl-2-(N-cyanoimino)thiazolidine into 6-Unsubstituted 2,4-Diamino-s-triazines by the Reaction with Amines
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3-Dimethoxymethyl-2-(N-cyanoimino)thiazolidine 1e reacts with secondary amines to afford 2,4-diamino-s-triazines 4 unexpectedly, while the triazine 5 bearing different amino groups at 2 and 4 positions is selectively obtained by the reaction with a mixture of two kinds of amines.
- Tanaka, Tetsuaki,Watanabe, Mayumi,Nakamoto, Yumi,Okuno, Kaori,Maekawa, Kaori,Iwata, Chuzo
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p. 2301 - 2302
(2007/10/02)
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- Synthesis of cimetidine and analogs thereof
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There is provided a process for producing cyanoguanidine derivatives, especially N-cyano-N'-Methyl-N"-(4-methyl-5-imidazolylmethyl)thioethyl-guanidine.
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- Synthesis of an imidazolyl isothiourea
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N-Cyano-N',S-ethylene-N'-([4-methyl-5-imidazolyl)methyl]isothiourea which is of value as an intermediate in the production of cimetidine and a process for its production are provided.
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- NEW SYNTHESES OF 2-CYANO-1-METHYL-3-THIO>ETHYL>GUANIDINE (CIMETIDINE)
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A new synthesis of 2-cyano-1-methyl-3-thio>ethyl>guanidine, 6 (cimetidine) utilizing the aziridine derivative 5 as a two-carbon one-nitrogen synthon, is reported.Attempts to prepare the key intermediate 5 via azirid
- Toso, Roberto,Mihalic, Mladen,Sega, Alessandro,Sunjic, Vitomir
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p. 345 - 350
(2007/10/02)
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