- A 6-hydroxy-5-nitro-nicotinic acid synthetic method and its separating and purifying method
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The invention discloses a synthetic method and a separation purification method of 6-hydroxyl-5-nitro niacin and belongs to the field of fine chemical engineering. According to the method, 6-hydroxyl niacin is used as a raw material and is subjected to pre-nitration reaction under the action of concentrated sulfuric acid, concentrated nitric acid and a catalyst ammonium bisulfate, nitration reaction, crystal separation purification and the like to obtain highly purified 6- hydroxyl-5-nitro niacin to meet purity requirements on midbody by pharmaceutical synthetic fields. The synthetic method has the advantages of being simple in synthetic process, mild in condition, high in yield, high in purity of obtained product, easy to operate and the like and is suitable for industrial production.
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Paragraph 0045-0064
(2018/02/04)
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- INDAZOLYL THIADIAZOLAMINES AND RELATED COMPOUNDS FOR INHIBITION OF RHO-ASSOCIATED PROTEIN KINASE AND THE TREATMENT OF DISEASE
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The invention provides indazolyl thiadiazolamines and related compounds, pharmaceutical compositions, methods of inhibiting Rho-associated protein kinase, and methods of treating inflammatory disorders, immune disorders, fibrotic disorders, and other medical disorders using such compounds. An exemplary indazolyl thiadiazolamine compound is an N-(5-[5-[(1H4ndazol-5-yl)amino]-1,3,4-thiadiazol-2-yl]pyridin-3-yl)acetamide compound.
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Paragraph 00372
(2016/09/22)
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- NOVEL COMPOUND, PRODUCTION METHOD THEREFOR, AND APPLICATION THEREFOR
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[Problems] To provide a novel peptide synthesis technique that is completely different than heretofore, and to provide a novel compound that enables the synthesis/creation of a novel artificial functional protein and the synthesis/creation of a novel functional peptide, as well as a method for producing the same. [Solution] A compound represented by formula (I) or a salt thereof.
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Paragraph 0188; 0190-0192
(2016/11/09)
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- NITROGENATED HETEROCYCLIC COMPOUND
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The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
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Paragraph 1032
(2015/03/28)
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- Development of a solid-supported biotinylation reagent for efficient biotin labeling of SH groups on small molecules
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We report here the design and synthesis of a novel and selective SH-group biotinylating reagent, KSH-1 (1), for the biotinylation of small molecules using solid phase chemistry. The results demonstrate that 1 efficiently biotinylated a small molecule, cap
- Fukumoto, Kentarou,Adachi, Kumi,Kajiyama, Akihiro,Yamazaki, Yuri,Yakushiji, Fumika,Hayashi, Yoshio
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supporting information; experimental part
p. 535 - 538
(2012/03/11)
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- Identification of a sulfonamide series of CCR2 antagonists
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A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pKa, yielded highly potent CCR2 antagonists exh
- Peace, Simon,Philp, Joanne,Brooks, Carl,Piercy, Val,Moores, Kitty,Smethurst, Chris,Watson, Steve,Gaines, Simon,Zippoli, Mara,Mookherjee, Claudette,Ife, Robert
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scheme or table
p. 3961 - 3964
(2010/09/03)
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- The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes
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This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
- Brooks, Gerald,Dabbs, Steven,Davies, David T.,Hennessy, Alan J.,Jones, Graham E.,Markwell, Roger E.,Miles, Timothy J.,Owston, Nathan A.,Pearson, Neil D.,Peng, Tony W.
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scheme or table
p. 5035 - 5037
(2011/01/04)
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- N3-substituted imidazopyridine c-Kit inhibitors
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Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
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Page/Page column 11; 14-15
(2008/06/13)
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- BICYCLIC IMIDAZOL DERIVATIVES AGAINST FLAVIVIRIDAE
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Disclosed are compounds, compositions and methods for treatingFlaviviridae family virus infections.
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Page/Page column 221
(2008/06/13)
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- N3-SUBSTITUTED IMIDAZOPYRIDINE C-KIT INHIBITORS
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Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
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Page/Page column 29
(2008/06/13)
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- Substituted triazolopyridine compounds
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A compound of formula wherein R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non- aromatic ring, containing no or one additional heteroatom selected from the group consiting of O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl; R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and n is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof. Compounds of formula I are useful in the treatment of disease associated with the adenosine A2 receptor.
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- Imidazopyridinone derivatives and their use as phosphodiesterase inhibitors
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A compound (Ia): wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc.
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- Solid phase synthesis of 1,3,5-trisubstituted pyridin-2-ones
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The solid phase synthesis of 1,3,5-trisubsituted pyridin-2-ones is reported via selective 1NH-alkylation of 3-amino-5-carbomethoxy-1H-pyridin- 2-one with a solid-supported halo-acid. Coupling of an acid to solid- supported 3-aminopyridinone was
- Linn, James A.,Gerritz, Samuel W.,Handlon, Anthony L.,Hyman, Clifton E.,Heyer, Dennis
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p. 2227 - 2230
(2007/10/03)
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- 5-arylindole derivatives
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Compounds of formula (I), wherein R 1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R 2, R 3, R 4 and R 5 are each independently hydrogen, C 1 to C 6 alkyl, aryl, C 1 to C 3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH 2) m NR 14 R 15, --(CH 2) m OR 9, --SR 9, --SO 2 NR 14 R 15, --(CH 2) m NR 14 SO 2 R 15 --(CH 2) m NR 14 CO 2 R 9, --(CH 2) m NR 14 COR 9, --(CH 2) m NR 14 CONHR 9, --CONR 14 R 15, or --CO 2 R 9 ; R 2 and R 3, R 3 and R 4, or R 4 and R 5 may be taken together to form a five- to seven-membered alkyl ring, a six-membered aryl ring, a five- to seven-membered heteroalkyl ring having 1 heteroatom of N, O, or S, or a five- to six-membered heteroaryl ring having H 1 or 2 heteroatoms of N, O, or S and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These compounds are useful psychotherapeutics and are potent serotonin (5-HT 1) agonists and benzodiazepine agonists and antagonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vosodilators. STR1
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