- NEW BIARYL AMIDE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 2
(2012/07/13)
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- NEW BIARYL AMIDE DERIVATIVES
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 53
(2012/07/14)
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- Creating an antibacterial with in vivo efficacy: Synthesis and characterization of potent inhibitors of the bacterial cell division protein FTSZ with improved pharmaceutical properties
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3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
- Haydon, David J.,Bennett, James M.,Brown, David,Collins, Ian,Galbraith, Greta,Lancett, Paul,MacDonald, Rebecca,Stokes, Neil R.,Chauhan, Pramod K.,Sutariya, Jignesh K.,Nayal, Narendra,Srivastava, Anil,Beanland, Joy,Hall, Robin,Henstock, Vincent,Noula, Caterina,Rockley, Chris,Czaplewski, Lloyd
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supporting information; experimental part
p. 3927 - 3936
(2010/09/04)
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- Practical synthesis of a potent bradykinin B1 antagonist via enantioselective hydrogenation of a pyridyl N-acyl enamide
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(Chemical Equation Presented) A practical and efficient synthesis of bradykinin B1 antagonist 1 is described. A convergent strategy was utilized which involved synthesis of three fragments: 3, 6, and 7. Cross coupling of fragments 6 and 7 followed by amidation with 3 enabled efficient synthesis of 1 in 19 steps total, a 35% overall yield from commercially available pyridine 10. The key to the success of the synthesis was the development of a fluorodenitration step to install the fluorine in pyridine 7 and a catalytic enantioselective hydrogenation of N-acyl enamide 9 to set the stereochemistry.
- O'Shea, Paul D.,Gauvreau, Danny,Gosselin, Francis,Hughes, Greg,Nadeau, Christian,Roy, Amelie,Shultz, C. Scott
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supporting information; experimental part
p. 4547 - 4553
(2009/09/30)
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- PYRIDYLAMIDINE COMPOUND OR SALT THEREOF, AND AGRICULTURAL OR HORTICULTURAL FUNGICIDE COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT
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An agricultural or horticultural fungicide composition having stabilized high plant disease control effect is provided. The agricultural or horticultural fungicide composition contains a pyridylamidine compound represented by the formula (I): or a salt th
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Page/Page column 16
(2009/09/04)
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- IMIDAZOPYRIDINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM
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The present invention relates to imidazopyridine analogs, methods of making imidazopyridine analogs, compositions comprising an imidazopyridine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising
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Page/Page column 31
(2009/04/24)
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- COMPOUNDS
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Bicyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 72-73
(2008/12/08)
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- ANTIBACTERIAL AGENTS
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Compounds of formula (I) have antibacterial activity wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is =C(R1)- or =N-; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are -CH2-, -CH2CH2-, -O-, or, in either orientation, -O- CH2- Or -OCH2CH2-; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, -N(CH2CH3)-, -C(=O)-, -O-(C=O)-, -C(=O)-O-, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, or -N(CH2CH3)-; and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.
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Page/Page column 124
(2010/11/28)
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- Bradykinin B1 antagonists: Biphenyl SAR studies in the cyclopropanecarboxamide series
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SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B1 antagonists was examined. Incorporation of a pyridine in place of the proximal phenyl ring and chlorination of the distal phenyl ring proved to be well tolerated
- Kuduk, Scott D.,DiPardo, Robert M.,Chang, Ronald K.,Di Marco, Christina N.,Murphy, Kathy L.,Ransom, Richard W.,Reiss, Duane R.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
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p. 3608 - 3612
(2008/02/08)
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- QUINAZOLINE DERIVATIVE
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This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R 1 represents a lower alkyl group et al; R 2 and R 3 are same and different and represents hydrogen atm et al; R 4 represents the substituent of the formula (II) et al; X 1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
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Page/Page column 76
(2010/11/25)
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- ASYMMETRIC HYDROGENATION OF ENAMIDES
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The present invention provides a process for the preparation of acyl amines of formula (I), enantiomerically enriched at the carbon atom marked with an *; wherein Y is N or CH; R1 and R2 are independently selected from H, halogen, C
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Page/Page column 7
(2010/11/30)
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- l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
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α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
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Page/Page column 19
(2008/06/13)
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- ALPHA-HYDROXY AMIDES AS BRADYKININ ANTAGONISTS OR INVERSE AGONISTS
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α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd.(4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or(b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra.and (7)(CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3-to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl;
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Page/Page column 28
(2008/06/13)
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- Synthesis and testing of new end-functionalized oligomers for molecular electronics
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Several new classes of oligomers have been synthesized with functionalities designed to aid in the understanding of molecular device behavior, specifically when molecules are interfaced between proximal electronic probes. The compounds synthesized are series of azobenzenes, bipyridines and oligo(phenylene vinylene)s that bear acetyl-protected thiols for ultimate attachment to metallic surfaces. Some initial electrochemical and solid-state test results are also reported.
- Flatt, Austen K.,Dirk, Shawn M.,Henderson, Jay C.,Shen, Dwanleen E.,Su, Jie,Reed, Mark A.,Tour, James M.
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p. 8555 - 8570
(2007/10/03)
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- 3-fluoropyridines, process for their preparation, and their use in liquid-crystal mixtures
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A 3-fluoropyridine of the formula (I) STR1 in which the symbols have the following meanings: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
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