ライフサイエンスコーパス: indazole

1 al acid-base property and tautomerization of indazole.

2 thylamine-mediated deoxygenation afforded 2H-indazoles.

3 en developed as a new practical synthesis of indazoles.

4 focused on a series of 3- and 4-substituted indazoles.

5 tained are useful precursors for indoles and indazoles.

6 benzyne leading to 1,3-dihydrothiazolo[3,4-b]indazoles.

7 ficient synthesis of N-vinyl- and C-vinyl-2H-indazoles.

8 This trend applies to various substituted indazoles.

9 onist YD-3 [1-benzyl-3(ethoxycarbonylphenyl)-indazole].

10 -aminoimidazole by a propylene linker at the indazole 1-position and to a diaminopropionate derivativ

11 -oxo-2-aryl-ethyl)-benzenesulfonamides to 2H-indazoles 1-oxides under mild conditions.

12 Base-catalyzed rearrangement of 2H-indazoles 1-oxides, prepared by tandem carbon-carbon fol

13 aminoethyl)-1-aryl-3,4-dihydropyrazino[1,2-b]indazole-2-ium 6-oxides rearranged to 2,3-dihydro-1H-imi

14 dazoles 25a and 25c versus the corresponding indazoles 25b and 25d.

15 s a chemoselective catalytic synthesis of 2H-indazoles, 2H-benzotriazoles, and related fused heterocy

16 i.e., 3-phenyl-3,3a,4,5-tetrahydro-2H-benz[g]indazoles, 3-phenyl-2,3,3a,4-tetrahydro[1]benzopyrano[4,

17 -1-ylcarbonyl)amino]-1-piperidinyl]ethyl]-1H-indazole-3- carboxamide) as a potent and selective 5-HT4

18 treating rats with 1-(2,4-dichlorobenzy)-1H-indazole-3-carbohydrazide (adjudin) to induce anchoring

19 h an acute dose of 1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide (adjudin, a male contraceptive

20 del using AF-2364 (1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide) to perturb Sertoli-germ cell

21 treated with AF-2364 [1-(2,4-dichlorobenzyl)-indazole-3-carbohydrazide] to perturb Sertoli-germ cell

22 he discovery of N-[(4-piperidinyl)methyl]-1H-indazole-3-carboxamide and 4-[(4-piperidinyl)methoxy]-2H

23 common N-[(1-alkylpiperidin-4-yl)methyl]-1H-indazole-3-carboxamide scaffold were prepared taking adv

24 A series of indole-3-carboxamides, indazole-3-carboxamides, and benzimidazolone-3-carboxami

25 cannabinoid methyl 2-(1-(4-fluorobenzyl)-1H-indazole-3-carboxamido)-3-methylbutanoate (AMB-FUBINACA,

26 t lonidamine (LND; 1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxylic acid) is known to interfere with e

27 very of an optimized and balanced inhibitor (indazole, 38).

28 and its cyclization to 3-(phenylethynyl)-3H-indazole 46b.

29 We probed different substitutions at the indazole 5-position and at the piperidine-nitrogen to ob

30 In N-(3,4-difluorophenyl-1H-indazole-5-carboxamide (30, PSB-1434, IC50 human MAO-B 1

31 ives were N-(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide (38a, PSB-1491, IC50 human MAO-B

32 bitors, namely 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides.

33 details the structure-guided optimization of indazole (6) using information gained from multiple liga

34 We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GP

35 teral injection of the NOS inhibitor 7-nitro indazole (7-NI) into the dorsolateral PAG cell columns p

36 tric oxide synthase (NOS), either by 7-nitro-indazole (7-NI) or N (G)-nitro-L-arginine methyl ester (

37 the nitric oxide synthase inhibitor 7-nitro indazole (7-NI), which does not block endothelial nitric

38 -L-arginine methyl ester (L-NAME) or 7-nitro indazole (7-NI).

39 the alpha,beta-unsaturated aldehydes and the indazole-7-carbaldehyde heterocycles were studied in ord

40 ion to its minimal pharmacophore provided an indazole acid lead compound.

41 c substrates including indole, indoline, and indazole afford the desired products in moderate to high

42 Indazole amide 3 was identified as a potent and selectiv

43 Identification of an indazole amide high throughput screening (HTS) hit follo

44 YC-1 [3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole], an HIF-1 inhibitor, reduced whole kidney glom

45 YC-1 [3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole], an NO-independent activator of sGC, produced

46 A series of 1-(2-aminopropyl)-1H-indazole analogues was synthesized and evaluated for the

47 um products generated from reactions between indazole and 4-chloro-1-methylpyridinium iodide under va

48 The endo-3-tropanamine derivatives in the indazole and benzimidazolone series possessed greater 5-

49 contain different hinge-binding "warheads": indazole and benzodioxole, respectively.

50 and regioselective synthesis of 2-methyl-2H-indazoles and 2-ethyl-2H-indazoles using trimethyloxoniu

51 nt, one-step benchtop syntheses of N-aryl-2H-indazoles and furans by C-H bond additions to aldehydes

52 The syntheses of both N-aryl-2H-indazoles and furans have been performed on 20 mmol scal

53 A series of unique indazoles and pyridoindolones have been rationally desig

54 tramolecularly to aryl substituents to yield indazoles and related compounds.

55 Indazole- and indole-carboxamides were discovered as hig

56 leading to enantioenriched fused polycyclic indazole architectures.

57 resence of strong base, however, N-protected indazoles are prone to an undesirable ring-opening react

58 Indazoles are regioselectively protected at N-2 by a 2-(

59 Indazoles are unselectively protected under strongly bas

60 terocycles, including indole, thiophene, and indazole, are tolerated.

61 A series of indazole arylsulfonamides were synthesized and examined

62 858R/T790M with inhibitors incorporating the indazole as hinge binder.

63 Our efforts concentrated on using an indazole as one of the P2 substituents since this group

64 ent Pd-catalyzed C-H functionalization of 2H-indazole at C3-position via an isocyanide insertion stra

65 Indazoles attached to a 2-aminopyridine or 2-aminoimidaz

66 merged from a phenotypic screen resulting in indazole-based compounds.

67 In contrast, indazole-based inhibitors exemplified by SR-3737 were po

68 ws for the reaction of variously substituted indazole, benzimidazole, pyrazole, indole, oxindole, and

69 In general, indoles, indazoles, benzotriazoles, indolones, and isatins gave a

70 ntified 1-benzyl-3-(3-dimethylaminopropyloxy)indazole (benzydamine, 3) as a potent activator of the n

71 a simple preparation of 3-oxy-substituted 2H-indazole, by an unrecognized method in the literature, i

72 study surrounding 3 clearly showed that the indazole C-3 dimethylaminopropyloxy substituent was crit

73 roxyl-containing groups were the more potent indazole C4 substituents.

74 Substituted 1H-indazoles can be formed from readily available arylimida

75 th N-substituted maleimides affording new 1H-indazoles characterized by an intense yellow color, a pr

76 elective estrogen receptor (ER) beta agonist indazole chloride (Ind-Cl) on functional remyelination i

77 These selectivity differences between the indazole class and the aminopyrazole class came despite

78 2E1 have been solved to 2.2 angstroms for an indazole complex and 2.6 angstroms for a 4-methylpyrazol

79 tion to produce a five-membered heterocyclic indazole complex, [((AdArO)3tacn)UIV(eta(2)-3-phen(Ind))

80 However, one indazole compound 33 was identified as a potent D1/D5 li

81 eening campaign identified 5-(2-chlorophenyl)indazole compound 4 as an antagonist of the transient re

82 Direct C7-arylation of 3-substituted 1H-indazole containing an EWG on the arene ring gave the ex

83 A new series of indazole-containing alpha(v)beta(3) integrin antagonists

84 ynthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homo

85 of nonsteroidal compounds having a phenyl-2H-indazole core with different groups at C-3.

86 ford N-unsubstituted indazoles or 1-arylated indazoles, depending upon the stoichiometry of the reage

87 ic aminocatalyzed aza-Michael addition of 1H-indazole derivatives to alpha,beta-unsaturated aldehydes

88 ide range of electrophiles to generate novel indazole derivatives.

89 ction of sterically congested dihydrobenzo[e]indazole derivatives.

90 A class of potent, nonsteroidal, selective indazole ether-based glucocorticoid receptor modulators

91 The fused polycyclic indazoles exhibit fluorescence properties and can underg

92 and artificial saliva, respectively, and the indazoles exhibited corresponding peaks at approximately

93 new class of azo photoswitches containing an indazole five-membered heterocycle shows photochemical i

94 Guided by X-ray co-crystal structures, indazole fragment 1 was elaborated to afford 12 (RMM-46)

95 h was observed in the direct preparations of indazoles from aldehydes.

96 n of thiazolo-, thiazino-, and thiazepino-2H-indazoles from o-nitrobenzaldehydes or o-nitrobenzyl bro

97 The fluorinated indazole group offers a handle for further functionaliza

98 ketones, acridones, acridinium salts, and 1H-indazoles has been developed starting from readily avail

99 lation procedure leading to C3,C7-diarylated indazoles has been developed.

100 A series of alkyne-linked bis-2H-indazoles has been prepared by the double cyclization of

101 mpounds containing either an isoquinoline or indazole heterocyclic core.

102 mined the crystal structures of three of the indazole hybrid compounds (CCG224061, CCG257284, and CCG

103 nitrogen heterocycles (pyrroles, pyrazoles, indazoles, imidazoles, and triazoles) was successfully p

104 ld primarily through the substitution of the indazole in 1 for a 2-aminopyrimidine.

105 arget thiazolo-, thiazino-, or thiazepino-2H-indazole in good overall yield.

106 tion affords the 3-hydroxymethyl-2-phenyl-2H-indazoles in good overall yield.

107 and pharmaceutically interesting substituted indazoles in good to excellent yields under mild reactio

108 Bicyclic indazole (IND) inhibited catalysis through a single CYP2

109 sulfonylpyridine (SAP), benzothiazole (BZT), indazole (IND), and tetrahydroindazole (THI) series as n

110 al structure of human JNK2 complexed with an indazole inhibitor by applying a high-throughput protein

111 ompatible synthesis of substituted N-aryl-2H-indazoles is reported via the rhodium(III)-catalyzed C-H

112 zation of o-nitrobenzylamines to 3-alkoxy-2H-indazoles is reported.

113 YC-1 [3-(5'-hydroxymethyl-2'furyl)-1-benzyl indazole] is an allosteric activator of soluble guanylyl

114 nd collection afforded a number of promising indazole leads which were truncated in order to identify

115 Further optimization of these indazoles led to the development of MLi-2 (1): a potent,

116 is proposed indicating the importance of the indazole ligands for binding site recognition and thus t

117 molecules revealing the dissociation of both indazole ligands from the ruthenium-based drug.

118 dan rigid moiety in a previously described N-indazole- N'-benzyl urea series led to a number of TRPV1

119 dium-catalyzed C-H borylation of N-protected indazoles occurs rapidly and selectively at C-3 and the

120 zomethane derivatives afford N-unsubstituted indazoles or 1-arylated indazoles, depending upon the st

121 YC-1 (3-[5'-Hydroxymethyl-2'-furyl]-1-benzyl-indazole), or vehicle three days before and seven days a

122 ntermediates that spontaneously dehydrate to indazole oxides.

123 The indazole-paroxetine analogs were indeed more potent than

124 xole-containing complexes confirmed that the indazole-paroxetine hybrids form stronger interactions w

125 The 2-aryl-2H-indazole products also represent a new class of readily

126 Indazoles represent a privileged scaffold in medicinal c

127 variety of substituents at position 5 of the indazole resulted in the potent inhibitor 20f (IC50 appr

128 arious substituents at the 6-position of the indazole ring greatly contributed to improvements in vit

129 However replacement of the indazole ring of 3 by appropriately substituted pyrazole

130 a are consistent with the model in which the indazole ring of granisetron interacts with Arg92 and th

131 In one model, the indazole ring of granisetron is near Trp90 and the tropa

132 optimization established the SAR around the indazole ring system, demonstrating that a trifluorometh

133 Indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (1, KP1019) and its analogue so

134 its analogue sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (2, KP1339) are promising redox

135 studied indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019) and its analogue sodiu

136 its analogue sodium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (NKP-1339).

137 NKP-1339 (sodium trans-[tetrachloridobis(1H-indazole)ruthenate(III)]), which is on the edge to clini

138 r ruthenium complex trans-[tetrachlorobis(1H-indazole)ruthenate(III)], otherwise known as KP1019, has

139 The 7-fluoro group on the indazole scaffold replaces the carbonyl group of an amid

140 idative transformations of 11 new indole and indazole SCs which are currently the predominant illicit

141 gration to afford 1-acyl or 1-alkoxycarbonyl indazoles selectively.

142 Using a previously disclosed indazole series of inhibitors as a starting point, and u

143 lidoacetamide "trigger" moiety within the C3 indazole series were also investigated.

144 report on the synthesis and evaluation of an indazole-spin-labeled compound that was designed as an e

145 Indazole substitution played a critical role in decreasi

146 sing imidazole, benzimidazole, pyrazole, and indazole substrates and poly(ethylene glycol) 400 (PEG40

147 These results suggest indazoles such as 13 may have an improved profile for po

148 neous resistant mutants generated against an indazole sulfonamide (GSK3011724A) identifies several sp

149 X-ray diffraction studies on two indazole sulfonamide fragments suggested the presence of

150 A new route to substituted 2-phenyl-2H-indazoles through the cyclization of (2-ethynylphenyl)ph

151 nt multidirectional syntheses of substituted indazoles to be realized.

152 s rearranged to 2,3-dihydro-1H-imidazo[1,2-b]indazoles under mild conditions.

153 esis of 2-methyl-2H-indazoles and 2-ethyl-2H-indazoles using trimethyloxonium tetrafluoroborate or tr

154 ond the ATP binding site, a potent series of indazoles was identified as selective pan-JAK inhibitors

155 A series of 3-aroyl indazoles was synthesized.

156 By employing unprotected indazoles with a free N-H bond, isomerization is averted

157 A novel direct C7-arylation of indazoles with iodoaryls is described using Pd(OAc)2 as

158 ryl group that allows for the preparation of indazoles without N-substitution.

159 We surmised from our prior studies that an indazole would be the stronger hinge binder and would im

160 ative 3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole (YC-1) is an allosteric stimulator of soluble g

161 steine, 3-(5-hydroxymethyl-2-furyl)-1-benzyl indazole (YC-1), and 8-bromo cGMP, all three of which ab

162 tecan, 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (YC-1), and flavopiridol.

163 ide or 3-(5'-hydroxymethyl-2'furyl)-1-benzyl-indazole (YC-1).

164 SAR studies of 3-substituted indazoles yielded analog 7 which demonstrated good in vi

165 Optimization of 4-substituted indazoles yielded two compounds, 27 and 48, that exhibit