- Synthesis, characterisation and crystal structure of a novel pyridyl urea Macrocycle
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A novel pyridyl urea based macrocycle has been synthesised and fully characterised including a single crystal X-ray structure determination. The synthetic approach first involves the reaction of benzyloxycarbonylaminopropyl-3-isocyanate with t-butyl 2-[(2-Aminopyridin-3- yl)oxy]acetate resulting in a coupling product. After deprotection of the amine and acid moieties and coupling subsequent coupling in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC), a macrocycle is formed. The structures of the compounds were confirmed by mass spectrometry and NMR spectroscopy. The X-ray crystal structure of the macrocycle reveals as expected a non-binding conformation with an intramolecular hydrogen bond between the urea NH and the pyridyl nitrogen.
- Areej, M. Al-Taweel,Perveen, Shagufta,Kilburn, Jeremy D.,Light, Mark E.
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p. 753 - 757
(2016/12/30)
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- SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS
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The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. wherein, ring D is Formula (a) or Formula (b): A and B, which may be same or different, are independently CR3 or N; Y is CR3 or N; L is selected from —NR2C(O)—, —C(O)NR2— and —NR2CRaRb—; Ra and Rb are independently hydrogen, halogen or substituted or unsubstituted alkyl; ring E is selected from the Formula (i) to (vii).
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Paragraph 0324
(2016/06/13)
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- A 2-amino-thiazole compounds (by machine translation)
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The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
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Paragraph 0605-0607
(2016/10/08)
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- FUSED IMIDAZOLE AND PYRAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 104; 126
(2015/06/25)
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- Short and efficient synthesis of oxazinone-and thiazinone-containing bicyclic heteroaromatic aldehydes
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Short and efficient route for the synthesis of oxazinone-and thiazinone-containing bicyclic heteroaromatic aldehydes, which involves the key step of palladium-catalyzed reductive carbonylation, is described. Overall routes for the synthesis of these aldehydes are short, versatile, and scalable with good yields of the product. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]
- Hameed P., Shahul,Shanbhag, Gajanan,Shinde, Vikas,Chinnapattu, Murugan,Manjrekar, Praveena,Puttur, Jayashree,Patil, Vikas,Ugarkar, Bheemarao
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p. 3315 - 3321
(2013/10/01)
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- A simple and facile route for the synthesis of 2H-1,4-benzoxazin-3-(4H)- ones via reductive cyclization of 2-(2-nitrophenoxy)acetonitrile adducts in the presence of Fe/acetic acid
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A simple route for the synthesis of 1,4-benzoxazin-3-(4H)-ones is described herein. This method involves the reductive cyclization of 2-(2-nitrophenoxy) acetonitrile adducts in the presence of Fe/acetic acid in good to excellent yields. This system was compatible with various other functional groups.
- Ramesh, Chintakunta,Raju, B. Rama,Kavala, Veerababurao,Kuo, Chun-Wei,Yao, Ching-Fa
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experimental part
p. 1187 - 1192
(2011/03/22)
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- [Omim][BF4], a green and recyclable ionic liquid medium for the one-pot chemoselective synthesis of benzoxazinones
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An efficient procedure for the one-pot chemoselective synthesis of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives from their corresponding o-aminophenols is developed using DBU in the ionic liquid [omim][BF4]. Upon completion of the reaction and separation of the product, the ionic liquid is recovered and successfully reused over nine recycles without any noticeable loss of performance.
- Sharifi, Ali,Barazandeh, Mehdi,Saeed Abaee,Mirzaei, Mojtaba
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experimental part
p. 1852 - 1855
(2010/09/07)
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- CYCLIC COMPOUNDS CONTAINING ZINC BINDING GROUPS AS MATRIX METALLOPROTEINASE INHIBITORS
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This invention provides compounds defined by Formula I Z-L-R1-Q-D-(V1)m-R2 I or a pharmaceutically acceptable salt thereof, wherein Z, L, R1, Q, D, V1, m, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.
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Page/Page column 256; 262
(2010/02/06)
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- Substituted pyrido[3,2-b]oxazin-3(4H)-ones: Synthesis and evaluation of antinociceptive activity
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A new series of N-substituted pyrido[3,2-b]oxazinones has been synthesized, pharmacologically evaluated, and compared with acetyl salicylic acid. The compound with the maximal combination of safety and analgesic efficacy was 4-{3-[4-(4-fluorophenyl-1-piperazinyl)propyl]}- 2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one (6c) with ED50 values of 12.5 mg/kg po (mouse: phenylquinone writhing test) and 27.8 mg/kg po (rat: acetic acid writhing test), respectively. Compound 6c proved to be more active than aspirin with a safety index of 5.1.
- Savelon,Bizot-Espiard,Caignard,Pfeiffer,Renard,Viaud,Guillaumet
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p. 133 - 142
(2007/10/03)
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