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Page 61

The glycine transporter type 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. We have recently discovered and developed [11C]RO5013853 as a novel positron emission tomog. tracer for GlyT1 for which a reliable five-step synthetic route was established. The incorporation of the radioisotope was achieved in the final step through methylation of a sodium sulfinate precursor, itself easily accessible upon redn. of the corresponding sulfonylchloride analog. [11C]RO5013853 was prepd. with high specific activity (>49 GBq/μmol) and high radiochem. purity (100%). A validation study of [11C]RO5013853 in animal imaging studies is in progress.

~3 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

79. Carboxylic acid derivatives having a 2,5,7-substituted oxazolopyrimidine ring

By Kadereit, Dieter; Schaefer, Matthias; Hachtel, Stephanie; Dietrich, Axel; Huebschle, Thomas; Gille, Andreas; Hiss, Katrin

From PCT Int. Appl. (2011), WO 2011086077 A1 20110721, Language: German, Database: CAPLUS

The invention relates to oxazolopyrimidine compds. of formula I as Edg-1 receptor activators, which are suitable for use in wound healing. Compds. of formula I wherein A is NH, O and S; X is C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc.; R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, etc.; R2 is (un)substituted Ph and (un)substituted 5- to 6-membered arom. monocyclic heterocycle; R3 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, etc.; R4 is H, C1-4 alkyl and C3-7 cycloalkyl-C0-2 alkyl; and stereoisomers, physiol. acceptable salts, solvates and solvates salts thereof, are claimed. Example compd. II was prepd. a multistep procedure (detailed procedure given). All the invention compds. were evaluated for their ability to activate Edg-1 receptor. From the assay, it was detd. that compd. II exhibited 100 % activation.

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Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

80. 3-[(6-Aminopyrimidin-4-yl)amino]benzenesulfonamide compounds useful as TNNI3K inhibitors, their preparation, and methods of use in the treatment of congestive heart failure

By Kallander, Lara S.; Lawhorn, Brian Griffin; Philip, Joanne; Zhao, Yongdong

From PCT Int. Appl. (2011), WO 2011088027 A1 20110721, Language: English, Database: CAPLUS

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Title compds. I are disclosed [wherein R1 = C1-4 alkyl; R2 = H, halo; R3 = H, halo, (un)substituted alkyl or alkoxy, aryl, OH, cycloalkyl, alkylthio, amino, (di)(alkyl)amino; R4 = H, halo, (un)substituted alkyl or alkoxy, OH, (halo)alkylthio, alkylsulfonyl, (un)substituted amino; R5 = H; or R4 and R5 form a 5 or 6 membered ring, optionally substituted or contg. one or two addnl. N/O/S atoms; R6 = alky(en/yn)yl, cycloalkyl, (un)substituted (hetero)aryl; and salts]. I are inhibitors of cardiac troponin I-interacting kinase (TNNI3K), also known as CARK (for cardiac ankyrin repeat kinase), a protein kinase that exhibits highly selective expression for cardiac tissues and which has been shown to interact with components of the sarcomere, including troponin I. Approx. 380 compds. I are claimed as the free base, and were prepd. as salts and/or free bases. Numerous intermediates were also prepd. For instance, the intermediate 3-[(6-chloro-4-pyrimidinyl)amino]-N- methylbenznesulfonamide and 3-biphenylamine were microwaved together in isopropanol in the presence of concd. HCl at 150° for 20 min to give invention compd. II, isolated as the trifluoroacetate. In bioassays using human TNNI3K, I exhibited pXC50 ³ approx. 6.0. For instance, two compds. I inhibited hTNNI3K with a mean pXC50 of approx. 7.0.

~0 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

81. Synthesis of a chiral stationary phase with poly[styrene-b-cellulose 2,3-bis(3,5-dimethylphenylcarbamate)] by surface-initiated atom transfer radical polymerization and its chiral resolution efficiency

By Yang, Ji-Hoon; Choi, Seong-Ho

From Journal of Applied Polymer Science (2011), 122(5), 3016-3022. Language: English, Database: CAPLUS, DOI:10.1002/app.34106

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A chiral stationary phase (CSP) with poly[styrene-b-cellulose 2,3-bis(3,5-dimethylphenylcarbamate)] was synthesized by the surface-initiated atom transfer radical polymn. (SI-ATRP) of cellulose 2,3-bis(3,5-dimethylphenylcarbamate)-6- acrylate after the SI-ATRP of styrene on the surface of silicon dioxide supports in pyridine. The successful prepn. of the CSP with poly[styrene-b-cellulose 2,3-bis(3,5-dimethylphenylcarbamate)] was confirmed via FTIR spectroscopy, field emission SEM, XPS, elemental anal., and thermal anal. The applicability for the chiral resoln. of the CSP with poly[styrene-b-cellulose 2,3-bis(3,5-diphenylcarbamate)] was evaluated with HPLC with 10 racemates under various mobile phases of hexane/alc., hexane/THF, and hexane/chloroform. The CSP with poly[styrene-b-cellulose 2,3-bis(3,5- diphenylcarbamate)] could be used in THF and chloroform as eluents. The chiral resolns. of the com. Chiracel OD, the CSP with cellulose 2,3-bis(3,5-dimethylphenylcarabmate), and the CSP with poly[styrene-b-cellulose 2,3-bis(3,5- dimethylphenylcarbamate)] prepd. by SI-ATRP were examd. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011.

~0 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

82. Synthesis of allylic trifluoromethyl ketones and their activity as inhibitors of the sex pheromone of the leopard moth, Zeuzera pyrina L. (Lepidoptera: Cossidae)

By Munoz, Lourdes; Bosch, M. Pilar; Batllori, Lluis; Rosell, Gloria; Bosch, Dolors; Guerrero, Angel; Avilla, Jesus From Pest Management Science (2011), 67(8), 956-964. Language: English, Database: CAPLUS, DOI:10.1002/ps.2139

BACKGROUND: Trifluoromethyl ketones (TFMKs), structurally related to the pheromones, are good inhibitors of pheromone communication in insects. To det. their activity on Zeuzera pyrina L. (Lepidoptera: Cossidae), a polyphagous pest, the authors have prepd. two diunsatd. TFMK analogs of the major and the minor pheromone components, and two monounsatd. ones. Their biol. activity in electroantennogram (EAG), wind tunnel and field tests is presented. RESULTS: The synthetic strategy to obtain the allylic TFMKs (E,Z)-1,1,1-Trifluoro-4,15-eicosadien-2-one and (E)-1,1,1-Trifluoro-4- eicosen-2-one is based on the reactions of (Z)-1,13-octadiene and 1-octadecene with trifluoroacetaldehyde Et hemiacetal, followed by Dess-Martin oxidn. of the resulting homoallylic trifluoromethyl alcs. In EAG, topical application of analogs (E,Z)-1,1,1-Trifluoro-4,15-eicosadien-2-one and (E,Z)-1,1,1-Trifluoro-5,15-eicosadien-2-one on male antennae significantly reduced the pheromone response. In the wind tunnel, (E,Z)-1,1,1-Trifluoro-5,15-eicosadien-2-one reduced the no. of contacts with the pheromone source. In the field, traps baited with mixts. of pheromone and inhibitors captured significantly fewer males than the pheromone alone. CONCLUSION: An efficient synthesis of allylic TFMKs is reported, with good overall yield, regiospecificity and diastereoselectivity. These compds. are good inhibitors of the pheromone in electrophysiol., wind tunnel and field tests. The results show the importance of two unsaturations at positions 2 and 13 of the trifluoroacyl group in the structure of the analogs, the latter being crit. for inhibitory activity. Copyright © 2011 Society of Chem. Industry.

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83. 4,6-Di-O-pentyl-3-O-trifluoroacetyl/propionyl cyclofructan stationary phases for gas chromatographic enantiomeric separations

By Zhang, Ying; Armstrong, Daniel W.

From Analyst (Cambridge, United Kingdom) (2011), 136(14), 2931-2940. Language: English, Database: CAPLUS, DOI:10.1039/c1an15205j

4,6-Di-O-pentyl-3-O-trifluoroacetyl cycloinulohexaose (DP-TA-CF6) and 4,6-di-O-pentyl-3-O-propionyl cycloinulohexaose (DP-PN-CF6) were synthesized and used as chiral stationary phases (CSPs) in gas chromatog. (GC). The chiral recognition ability of the two CSPs was studied. A total of 47 racemic compds. were sepd. on the two new CSPs, including derivatized amino acids, amino alcs., amines, alcs., tartrates and lactones. Several analytes were only sepd. on either the DP-TA-CF6 or the DP-PN-CF6 phase. The chiral recognition mechanism was evaluated through thermodn. anal. The result indicated there was no inclusion complex formation involved in the chiral recognition process.

~3 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

84. Pyrrolidine derivatives as NK-3 receptor antagonists and their preparation, pharmaceutical compositions and use in the treatment of diseases

By Knust, Henner; Koblet, Andreas; Nettekoven, Matthias; Ratni, Hasane; Riemer, Claus; Vifian, Walter From U.S. Pat. Appl. Publ. (2011), US 20110144081 A1 20110616, Language: English, Database: CAPLUS

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The invention relates to pyrrolidine derivs. of formula I and their pharmaceutically active salts. Compds. of formula I are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD). Compds. of formula I wherein each R1 is independently H, halo, CN and lower (halo)alkyl; n is 1-3; R2 is H and Me; R3 is (CH2)1-2-CONH2, (CH2)1-2-CN, (un)substituted non-arom. heterocyclic group, etc.; Z is O, NH and N(lower alkyl); R4 is (un)substituted lower alkyl, -(CH2)2-3-lower alkyl, - CH(CH3)CH2-lower alkoxy, -(CH2)0-3-CN, bicyclo[2.2.1]heptyl, etc.; and their pharmaceutically active salts thereof, are claimed. Example compd. II was prepd. via hydrolysis of rac- {(3R,4S)-4-(3,4-dichlorophenyl)-1-[1-(1- methylcyclopropylcarbonyl)piperidin-4-carbonyl]pyrrolidin-3- yl}(methyl)carbamic acid tert-Bu ester; the resulting rac-{4- [(3S,4R)-3-(3,4-dichlorophenyl)-4-(methylamino)pyrrolidine-1- carbonyl]piperidin-1-yl}-(1- methylcyclopropylcarbonyl)methanone underwent acylation with 4-fluorophenyl chloroformate to give II. All the invention compds. were evaluated for their NK-3 receptor antagonistic activity. From the assay, it was detd. that compd. II exhibited the IC50 value of 4 nM.

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85. Preparation of 2-amino-3-arylpropanoic acid and 2-amino-3-heterocyclylpropanoic acid derivatives as tryptophan hydroxylase inhibitors for the treatment of cancer

By Oravecz, Tamas

From PCT Int. Appl. (2011), WO 2011056916 A1 20110512, Language: English, Database: CAPLUS

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The title compds. [I; A = each optionally substituted cycloalkyl, aryl, or heterocycle; X = a bond, O, S, C(O), C(R4):, :C(R4), C(R3R4), C(R4):C(R4), CºC, N(R5), N(R5)C(O)N(R5), C(R3R4)N(R5), N(R5)C(R3R4), ONC(R3), C(R3)NO, C(R3R4)O, OC(R3R4), SO2, SO2N(R5), N(R5)SO2, C(R3R4)SO2, or SO2C(R3R4); D = each optionally substituted aryl or heterocycle; R1 = H or each optionally substituted alkyl, alkylaryl, alkylheterocycle, aryl, or heterocycle; R2 = H or ech optionally substituted alkyl, alkylaryl, alkylheterocycle, aryl, or heterocycle; R3 = H, alkoxy, amino, cyano, halogen, hydroxy, or optionally substituted alkyl; R4 = H, alkoxy, amino, cyano, halogen, hydroxy, or optionally substituted alkyl or aryl; R5 = independently H or each optionally substituted alkyl or aryl; n = 0-3] or pharmaceutically acceptable salts thereof are prepd. These compds. such as (2S)-2-amino-3-[4-(pyrimidin-4-yl)phenyl]propanoic acid derivs., (S)-2-amino- 3-[4-(1,3,5-triazin-2-yl)phenyl]propanoic acid derivs., and 2-amino-3-[3-(1,3,5-triazin-2-yl)-1H-pyrazol-1-yl]propanoic acid derivs. are useful as inhibitors of tryptophan hydroxylase such as human tryptophan hydroxylase type II (TPH2) and human tryptophan hydroxylase type I (TPH1) (no data). Methods and compns. for the treatment and/or management of cancer such as serotonin-producing tumor, breast cancer, cholangiocarcinoma, and neuroendocrine tumor, and prostate cancer, are disclosed, which comprise the use of tryptophan hydroxylase inhibitors I. Thus, addn. reaction of 3,4- difluorobenzaldehyde with (trifluoromethyl)trimethylsilane in the presence of tetrabutylammonium fluoride in THF at room temp. for 4 h followed by treating the reaction mixt. with 1 M aq. HCl soln. overnight gave 90% 1-(3,4-difluorophenyl)- 2,2,2-trifluoroethanol (II). II was treated with NaH in THF at room temp. for 20 min and underwent etherification with 4,6- dichloropyrimidine at 70° for 1 h to give 70% 4-chloro-6-[1-(3,4-difluorophenyl)-2,2,2-trifluoroethoxy]pyrimidine(III). Coupling of III with 4-borono-L-phenylalanine in the presence of 5 mol% dichlorobis(triphenylphosphine)palladium(II) in a mixt. of 70% aq. MeCN and 1 M aq. NaOH soln. under heating at 150° for 5 min by microwave gave 21% (2S)-2-amino- 3-[4-[6-[1-(3,4-difluorophenyl)-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid (IV).

~2 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

86. Preparation of quinazoline derivatives as TNNI3K inhibitors useful for treating congestive heart failure

By Kallander, Lara S.; Lawhorn, Brian Griffin; Philp, Joanne

From PCT Int. Appl. (2011), WO 2011056740 A1 20110512, Language: English, Database: CAPLUS

Title compds. I [R1 = alkyl; R2 = H or halo; R3 = H, halo, alkyl, etc.; R4 = H; R5, R6 and R7 independently = H, halo, NO2, etc.], and their pharmaceutically acceptable salts, are prepd. and disclosed as cardiac troponin I-interacting kinase (TNNI3K) inhibitors. Thus, e.g., II was prepd. by condensation reaction of 3-amino-4-(dimethylamino)-N- methylbenzenesulfonamide with 4-chloro-6,7-bis(methyloxy)quinazoline. All the exemplar compds. inhibited hTNNI3K ATP binding in fluorescent polarization assay with a pXC50 value ³ 6.0. I are useful for treating congestive heart failure.

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~0 Citings

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87. Preparation of 2-(pyridin-4-yl)benzoxazole derivatives and their composition and method for controlling arthropod pests

By Otsuki, Junko

From PCT Int. Appl. (2011), WO 2011049223 A1 20110428, Language: English, Database: CAPLUS

The invention provides an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. of formula (I) and pyridalyl; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and pyridalyl to the arthropod pests or a locus where the arthropod pests inhabit; and so on. Compds. of formula I wherein A1 and A2 are independently N and CR7; R1 and R4 are independently halo and H; R2 and R3 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, (un)substituted Ph, etc.; R5 and R6 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, halo, H, etc.; R5R6 may be taken together to form (un)substituted 5- to 6-membered ring; R7 is (un)substituted C1-3 alkyl, (un)substituted C1-3 alkoxy, CN, halo and H; n is 0 and 1; are claimed. Example compd. (II) was prepd. by cyclocondensation of isonicotinic acid with 2-amino-4-propylphenol. All the invention compds. were evaluated for their pesticidal activity (some data given).

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~0 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

88. Preparation of 2-(pyridin-4-yl)benzoxazole derivatives and their composition and method for controlling arthropod pests

By Otsuki, Junko

From PCT Int. Appl. (2011), WO 2011049222 A1 20110428, Language: English, Database: CAPLUS

The present invention provides: an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. and a diamide compd.; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and a diamide compd. to the arthropod pests or a locus where the arthropod pests inhabit; and so on. The invention provides an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. of formula (I) and a diamide compd.; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and a diamide compd. to the arthropod pests or a locus where the arthropod pests inhabit; and so on. Compds. of formula I wherein A1 and A2 are independently N and CR7; R1 and R4 are independently halo and H; R2 and R3 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, (un)substituted Ph, etc.; R5 and R6 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, halo, H, etc.; R5R6 may be taken together to form (un)substituted 5- to 6-membered ring; R7 is (un)substituted C1-3 alkyl, (un)substituted C1-3 alkoxy, CN, halo and H; n is 0 and 1; are claimed. Example compd. (II) was prepd. by cyclocondensation of isonicotinic acid with 2-amino-4- propylphenol. All the invention compds. were evaluated for their pesticidal activity (some data given).

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~1 Citing

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

89. Preparation of 2-(pyridin-4-yl)benzoxazole derivatives and their composition and method for controlling arthropod pests

By Otsuki, Junko

From PCT Int. Appl. (2011), WO 2011049221 A1 20110428, Language: English, Database: CAPLUS

The invention provides an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. of formula (I) and a pyrethroid compd.; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and a pyrethroid compd. to the arthropod pests or a locus where the arthropod pests inhabit; and so on. Compds. of formula I wherein A1 and A2 are independently N and CR7; R1 and R4 are independently halo and H; R2 and R3 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3- 6 alicyclic hydrocarbon, (un)substituted Ph, etc.; R5 and R6 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, halo, H, etc.; R5R6 may be taken together to form (un)substituted 5- to 6- membered ring; R7 is (un)substituted C1-3 alkyl, (un)substituted C1-3 alkoxy, CN, halo and H; n is 0 and 1; are claimed. Example compd. (II) was prepd. by cyclocondensation of isonicotinic acid with 2-amino-4-propylphenol. All the invention compds. were evaluated for their pesticidal activity (some data given).

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~2 Citings

Copyright © 2014 American Chemical Society (ACS). All Rights Reserved.

90. Preparation of 2-(pyridin-4-yl)benzoxazole derivatives and their composition and method for controlling arthropod pests

By Otsuki, Junko

From PCT Int. Appl. (2011), WO 2011049220 A1 20110428, Language: English, Database: CAPLUS

The present invention provides: an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. and pyriproxyfen; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and pyriproxyfen to the arthropod pests or a locus where the arthropod pests inhabit; and so on. The invention provides an arthropod pests control compn. comprising, as active ingredients, a condensed heterocyclic compd. of formula (I) and pyriproxyfen; a method for controlling arthropod pests which comprises applying effective amts. of a condensed heterocyclic compd. and pyriproxyfen to the arthropod pests or a locus where the arthropod pests inhabit; and so on. Compds. of formula I wherein A1 and A2 are independently N and CR7; R1 and R4 are independently halo and H; R2 and R3 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, (un)substituted Ph, etc.; R5 and R6 are independently (un)substituted C1-6 acyclic hydrocarbon, (un)substituted C3-6 alicyclic hydrocarbon, halo, H, etc.; R5R6 may be taken together to form (un)substituted 5- to 6-membered ring; R7 is (un)substituted C1-3 alkyl, (un)substituted C1-3 alkoxy, CN, halo and H; n is 0 and 1; are claimed. Example compd. (II) was prepd. by cyclocondensation of isonicotinic acid with 2-amino-4- propylphenol. All the invention compds. were evaluated for their pesticidal activity (some data given).

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