- OXADIAZOLE MODULATORS OF S1P METHODS OF MAKING AND USING
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The invention is directed to Compounds of Formula (I): wherein each variable is defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance for treating graft versus host disease and autoimmune diseases.
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Paragraph 0164
(2017/01/23)
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- THIADIAZOLE MODULATORS OF S1P AND METHODS OF MAKING AND USING
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The invention is directed to compounds of the formula: wherein each of the variables are defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance treating an autoimmune disease.
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Paragraph 0235
(2017/01/26)
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- SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS GPR120 AGONISTS
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The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related di
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Page/Page column 150
(2017/12/29)
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- HERBICIDES
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The present invention relates to herbicidally active pyridino-/pyrimidino-pyridine derivatives. The invention further provides processes and intermediates used for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, as well as to the use of such compounds and compositions in controlling undesirable plant growth: in particular the use in controlling weeds, in crops of useful plants.
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Page/Page column 43
(2017/10/30)
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- 6-chloro-3-fluoro-2-pyridine carboxylic acid synthesis
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The invention discloses a 6-chlorine-3-fluorine-2-picolinic acid synthesis process. The main starting material is 6-chlorine-3-fluorine-2-methylpyridine.The 6-chlorine-3-fluorine-2-methylpyridine serves as the starting material, dilute sulphuric acid is a solvent, potassium dichromate is an oxidizing agent, sodium tungstate (Na2WO4 2H2O) and crown ether are a composite catalyst, after reaction is completed, a crude product is obtained through conventional post-processing, the crude product is heated to be dissolved in an alkaline aqueous solution, unreacted micro raw materials and other impurities are extracted through an organic solvent, a water layer is acidized through mineral acid, pure 6-chlorine-3-fluorine-2-picolinic acid is obtained after cooling and crystallization are carried out, the yield is high, and the quality of the product is good.
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Paragraph 0026-0027
(2017/03/14)
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- Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: Effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice
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Analogs of A-98593 (1) and its enantiomer ABT-594 (2) with diverse substituents on the pyridine ring were prepared and tested for affinity to nicotinic acetylcholine receptor binding sites in rat brain and for analgesic activity in the mouse hot plate assay. Numerous types of modifications were consistent with high affinity for [3H]cytisine binding sites. By contrast, only selected modifications resulted in retention of analgesic potency in the ame range as 1 and 2. Analogs of 2 with one or two methyl substituents at the 3-position of the azetidine ring also were prepared and found to be substantially less active in both assays.
- Holladay, Mark W.,Bai, Hao,Li, Yihong,Lin, Nan-Horng,Daanen, Jerome F.,Ryther, Keith B.,Wasicak, James T.,Kincaid, John F.,He, Yun,Hettinger, Anne-Marie,Huang, Peggy,Anderson, David J.,Bannon, Anthony W.,Buckley, Michael J.,Campbell, Jeffrey E.,Donnelly-Roberts, Diana L.,Gunther, Karen L.,Kim, David J. B.,Kuntzweiler, Theresa A.,Sullivan, James P.,Decker, Michael W.,Arneric, Stephen P.
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p. 2797 - 2802
(2007/10/03)
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- Synthesis of dihalopicoline N-oxides and their 4-nitro derivatives
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Three aminohalo-substituted α- and β-picolines, six dihalo-substituted α- and β-picolines, six dihalo-substituted α- and β-picoline N-oxides and six respective dihalo-4-nitropicoline N-oxides were synthesized in excellent yields. Some properties of the products were reported. 1997 Plenum Publishing Corporation.
- Ciurla,Puszko
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p. 1173 - 1177
(2007/10/03)
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- Pyrido[3,2-e][1,4]diazepines - Synthesis and anti-HIV-1-activity tests
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Starting from the commercially available 6-methyl-2-pyridylamine (1) the pyrido[3,2-e][1,4]diazepine 14a was synthesized in 12 steps with 7% total yield. 14a, the N-methyl derivative 14b, the thiolactam 15a, the amidine 16, and the 1,2,4-triazole 17 were tested for anti-HIV-1-activity. None of the compounds tested possesses antiviral activity comparable to that of zidovudine (3'-azido-3'-desoxythymidine = AZT).
- Gorlitzer,Wilpert,Rubsamen-Waigmann,Suhartono,Wang,Immelmann
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p. 247 - 255
(2007/10/02)
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