- Synthetic method of medical intermediate cycloalkanopyrimidinedione compound
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The invention provides a synthetic method of a cycloalkanopyrimidinedione compound, and belongs to the technical field of organic synthesis. The method provided by the invention comprises the following steps of: taking a 2-methoxycarbonyl naphthenone comp
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Paragraph 0020-0022
(2020/12/15)
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- 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 00247-00250
(2017/05/31)
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- BICYCLIC DERIVATIVE CONTAINING PYRIMIDINE RING, AND PREPARATION METHOD THEREFOR
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The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.
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Paragraph 0238
(2016/04/26)
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- Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor
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A series of novel 2-amino-4-pyrazolecyclopentylpyrimidines have been prepared and evaluated as IGF-1R tyrosin kinase inhibitors. The in vitro activity was found to depend strongly on the substitution pattern in the 2-amino ring, 4-pyrazolo moieties and size of fused saturated ring with the central pyrimidine core. A stepwise optimization by combination of active fragments led to discovery of compound 6f and 6k, two structures with IGF-1R IC50 of 20 nM and 10 nM, respectively. 6f was further profiled for its anti cancer activity across various cell lines and pharmacokinetic studies in Sprague Dawley rats.
- Aware, Valmik,Gaikwad, Nitin,Chavan, Sambhaji,Manohar, Sonal,Bose, Julie,Khanna, Smriti,B-Rao, Chandrika,Dixit, Neeta,Singh, Kishori Sharan,Damre, Anagha,Sharma, Rajiv,Patil, Sambhaji,Roychowdhury, Abhijit
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supporting information
p. 246 - 256
(2015/05/26)
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- Carboxylic acid derivatives, their preparation and use in treating cancer
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This invention provides a method for treating cancer in an individual, wherein the cancer is a tumor in which endothelin is upregulated (e.g. tumors of the prostate, lung, liver, breast, brain, stomach, colon, endometrium, testicle, thyroid, pituatary, bladder, kidney, pancreas and meninges) by administering to the individual an effective amount of a compound of Formula I or Formula Ia, as describe herein.
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- Pyrimidine Derivatives. II. New Synthesis and Reactions of 4-Amino-2-methylthiopyrimidine Derivatives
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4-Amino-2-methylthiopyrimidine derivatives (4) were synthesized by the cyclization of 3-cyano-2-methylisothiourea (2) with ketones (3).Oxidation of 4 produced 4-amino-2-methylsulfinyl or 2-methylsulfonylpyrimidine derivatives (7 or 8).Amination of 7 or 8 gave hypoglycemic 2-(1-piperazinyl)pyrimidines (1).Compounds 4 were converted to 4(3H)-pyrimidinone derivatives (12).Derivatives 1 were also synthesized via 12.Keywords - hypoglycemic drug; base-catalyzed cyclization; 3-cyano-2-methylisothiourea; 4-amino-2-methylthiopyrimidines; 4-amino-2-methylthio-5,6,7,8-tetrahydroquinazoline; 2-methylthio-4(3H)-pyrimidinones; 2-methylsulfinylpyrimidines amination; 2-methylsulfonylpyrimidines amination
- Sekiya, Tetsuo,Hiranuma, Hidetoshi,Uchide, Masayuki,Hata, Shunsuke,Yamada, Shun-Ichi
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p. 948 - 954
(2007/10/02)
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