- Steric effects in the catalytic amination of γ-, δ-, and ε-glycols
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The amination of butane-1,4-diol, isomeric dipropylene glycols, and cyclohexane-1,4-diyldimethanol in the presence of nickel/copper/chromium catalysts has been studied. The effect of the initial glycol structure on the reaction selectivity has been estima
- Timofeev,Bazanov,Zubritskaya
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p. 1756 - 1761
(2017/02/19)
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- NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
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Paragraph 00289
(2013/12/03)
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- TRICYCLIC TETRAHYDROQUINOLINE ANTIBACTERIAL AGENTS
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The invention includes tetrahydroquinoline and related compounds of formula (I), and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.
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- Imidazole derivatives
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The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
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- 3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants and antiepileptics
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Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: STR1 wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R1 and R2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R1 and R2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R1 and R2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by fluoro, loweralkyl, loweralkoxy, trifluoromethyl, acetyl, or aminocarbonyl, then R1 and R2 cannot both be hydrogen.
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- Alicyclic Nitrosamines and Nitrosamino Acids as Transnitrosating Agents
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Many alicyclic nitrosamines act as nitrosating agents under mild conditions (pH 1-3, in the presence of nucleophilic catalysts such as thiocyanate).All nitrosopiperazines, nitrosomorpholines, and nitrosamino acids tested were found to act as nitrosating agents, and certain nitrosopiperidines also showed this capability.Acyclic nitrosamines are far less reactive than functionally similar cyclic compounds.
- Singer, Sandra S.,Singer, George M.,Cole, Barbara B.
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p. 4931 - 4935
(2007/10/02)
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