ライフサイエンスコーパス: indazole

1 t intermediate, we had need of a fluorinated indazole.

2 inophosphonium substituted by a zwitterionic indazole.

3 al acid-base property and tautomerization of indazole.

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

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

6 This trend applies to various substituted indazoles.

7 thylamine-mediated deoxygenation afforded 2H-indazoles.

8 en developed as a new practical synthesis of indazoles.

9 nables functionalization of the 3-alkenyl-2H-indazoles.

10 radical to the ortho position of 1-phenyl-1H-indazoles.

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

12 tained are useful precursors for indoles and indazoles.

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

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

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

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

17 3-azoles predicts the reactivities of N-aryl indazoles, 1,2,4-triazolopyrazines, 1,2,3-thiadiazoles,

18 e cyclization of N-phenylnitrile imine 13 to indazole 17.

19 -ortho-aroylation of substituted 1-phenyl-1H-indazoles 1a-j with various substituted aldehydes 3a-t v

20 o[2,1-b]thiazole, imidazo[2,1-b]thiazole, 2H-indazole, 1H-indazole, 1H-pyrazole, and 1,2,4-oxadiazol-

21 ole, imidazo[2,1-b]thiazole, 2H-indazole, 1H-indazole, 1H-pyrazole, and 1,2,4-oxadiazol-5(4H)-one as

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

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

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

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

26 -1-ylcarbonyl)amino]-1-piperidinyl]ethyl]-1H-indazole-3- carboxamide) as a potent and selective 5-HT4

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

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

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

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

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

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

33 can broadly recognize various members of the indazole-3-carboxamide synthetic cannabinoid family.

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

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

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

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

38 od that results in (C-2')-cyanated 2-aryl-2H-indazoles 3a-j, (C-2')-cyanated 1-aryl-1H-indazoles 4a-j

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

40 2H-indazoles 3a-j, (C-2')-cyanated 1-aryl-1H-indazoles 4a-j [distal], or C-3 cyanated 2-aryl-2H-indaz

41 of monosubstituted o-benzoyl/acyl-1-aryl-1H-indazoles 4a-t/5a-i and bis-substituted o-benzoyl-1-aryl

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

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

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

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

46 les 4a-j [distal], or C-3 cyanated 2-aryl-2H-indazoles 5a-i [proximal] products in good to excellent

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

48 activation/[4 + 2] annulation of 2-benzyl-2H-indazole-6-carboxylic acids with ynamides, enabling the

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

50 5a-i and bis-substituted o-benzoyl-1-aryl-1H-indazoles 6a-j in <=88% yields.

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

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

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

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

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

56 st but harsh method for the synthesis of 2 H-indazoles, a valuable class of nitrogen heterocycles.

57 c index (PI) to 6600, while N-methylation of indazole abolished the PI increasing dark toxicity, thus

58 The 2H-tautomer of indazole absorbs light more strongly than the 1H-tautome

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

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

61 The calculations suggest that the indazole allylation reaction proceeds through an enantio

62 Indazole amide 3 was identified as a potent and selectiv

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

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

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

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

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

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

69 Irreversible indazole and benzimidazolylidene (BIY) linkages are intr

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

71 e pivotal role of the dual directing groups (indazole and carboxylic acid) in facilitating selective

72 o explain the reactivity differences between indazole and indole electrophiles, the latter of which w

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

74 onalized dihydroquinazolines from 2,3-diaryl-indazoles and acetonitrile involving the same electroche

75 catalyzed energy transfer process between 2H-indazoles and alpha-keto acids, offering advantages like

76 A series of formylated indazoles and carboxylic acid esters of indazole derivat

77 H cross-dehydrogenative coupling between 2 H-indazoles and ethers has been achieved using a catalytic

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

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

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

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

82 formation of fulvenallene and fluorenes from indazoles and the corresponding formation of azafulvenal

83 eta-carbolin triazoles, imidazole, pyrazole, indazole, and tetrazole) and porphyrins to access divers

84 on of a variety of functionalized pyrazoles, indazoles, and aromatics.

85 evant heteroaryls such as indoles, pyrroles, indazoles, and azaindoles.

86 s, including purines, tetrazoles, triazoles, indazoles, and benzo-fused congeners, undergo regio- and

87 Indazole- and indole-carboxamides were discovered as hig

88 leading to enantioenriched fused polycyclic indazole architectures.

89 Indoles and indazoles are common moieties in pharmaceuticals and nat

90 operties of the synthesized 3-substituted-1H-indazoles are investigated, and some of them showed very

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

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

93 Methods for direct C3-functionalization of indazoles are relatively rare, compared to reactions dev

94 ition is known to occur in low yield when 1H-indazoles are subjected to high-energy UVC irradiation.

95 Indazoles are unselectively protected under strongly bas

96 C3-substituted 1H-indazoles are useful and important substructures in many

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

98 A series of indazole arylsulfonamides were synthesized and examined

99 858R/T790M with inhibitors incorporating the indazole as hinge binder.

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

101 ation and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen recepto

102 ring closing, initiating from cinnolines and indazoles as designed precursors.

103 rt the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD

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

105 A substituted indazole at pyrazole position 3 results in novel interac

106 3-H sulfonylation of biologically diverse 2H-indazoles at room temperature and under ambient air.

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

108 inopiperidine linkers in combination with an indazole-based cereblon (CRBN)-binding moiety (CBM).

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

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

111 The results suggest that irradiation of the indazole-based Ir(III) complex leads to PCET involving t

112 These aptamers can recognize many indazole-based synthetic cannabinoids with high affinity

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

114 idazole, pyrazole, indole, azindole, purine, indazole, benzimidazole, pyridone, carbazole), providing

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

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

117 The indazole bioisosteres 10 and 11 showed higher metabolic

118 of C-phenylnitrile imine 19 can also lead to indazole, but this reaction, which passes through a carb

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

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

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

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

123 time that the 2H tautomers of 3-substituted indazoles can be stabilized by an intermolecular hydroge

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

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

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

127 2E1 have been solved to 2.2 angstroms for an indazole complex and 2.6 angstroms for a 4-methylpyrazol

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

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

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

131 w cell were used to obtained 3-(arylthio)-2H-indazole compounds on a gram scale within the residence

132 lash vacuum pyrolysis (FVP) of pyrazoles and indazoles constitutes a valuable route to carbenes and n

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

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

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

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

137 ctively cleaves the N-N bond of pyrazole and indazole cores to afford pyrimidines and quinazolines, r

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

139 or bis-aroylation of substituted 1-phenyl-1H-indazoles depends on the type of oxidant being used for

140 sulfonyl precursor, a series of sulfonylated indazole derivatives containing a broad spectrum of func

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

142 3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selec

143 ated indazoles and carboxylic acid esters of indazole derivatives were produced in moderate to excell

144 mation provides direct access to fluorinated indazole derivatives with broad functionalities in satis

145 ide range of electrophiles to generate novel indazole derivatives.

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

147 for the direct synthesis of 3-substituted-1H-indazole employing p-quinone methide (p-QM) and arylhydr

148 Systematic tuning from imidazole to indazole enhanced the phototherapeutic index (PI) to 660

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

150 The fused polycyclic indazoles exhibit fluorescence properties and can underg

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

152 Also, the synthesized 3-substituted-1H-indazole exhibits an acid-sensitive fluorescence turn-of

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

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

155 zed intramolecular synthesis of 3-alkenyl-2H-indazoles from 2-alkynylazobenzenes is described.

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

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

158 carbenes cyclize very easily to 2 H- and 3 H-indazoles, from which 6-methylenecyclohexadienylidene, p

159 approach for accessing structurally diverse indazole-fused pyran derivatives under mild reaction con

160 es, enabling the regioselective synthesis of indazole-fused pyrans.

161 A facile synthesis of novel indazole-fused pyrazoles from pyrazol-3-ones and alkynoa

162 ted tetrahydroisoquinoline scaffold, with an indazole group led to the removal of a reactive metaboli

163 The fluorinated indazole group offers a handle for further functionaliza

164 ndly protocol for the arylselenylation of 2H-indazole has been developed using a catalytic amount of

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

166 t, simple, and metal-free fluorination of 2H-indazoles has been developed using N-fluorobenzenesulfon

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

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

169 A variety of C-3 oxyalkylated 2 H-indazoles have been synthesized in moderate to good yiel

170 mpounds containing either an isoquinoline or indazole heterocyclic core.

171 ermeability compared to that of the original indazole hinge binding scaffold, while maintaining poten

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

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

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

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

176 itrochalcones with pyrazoles, imidazole, and indazole in the presence of CuI catalyst, DBU base, and

177 approach to a library of trifluoromethylated indazoles in 35-83% yields.

178 a sealed tube delivers the 2-substituted-2H-indazoles in a single synthetic step with yields up to 7

179 a sealed tube delivers the 2-substituted-2H-indazoles in a single synthetic step with yields up to 7

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

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

182 hetically important diverse 3-substituted-1H-indazoles in good yields.

183 Thirty-nine halogenated pyrazoles and indazoles, including pharmaceuticals such as celecoxib,

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

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

186 dig cyclization to achieve a wide variety of indazole-indole hybrids in good yields.

187 thesis of a diverse range of C-3-substituted indazole-indole hybrids using readily accessible 2-(indo

188 range of substrates was examined, including indazoles, indoles, pyrazoles, and benzimidazole, featur

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

190 ive C-S bond coupling of aryl thiols with 2H-indazole is reported.

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

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

193 selective synthesis of 2-aryl-substituted 2H-indazoles is reported.

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

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

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

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

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

199 se by exploiting the unique properties of an indazole metastable-state photoacid (mPAH).

200 through the control of C3 nucleophilicity of indazole moiety.

201 Here, 2 H-indazole N-oxides were synthesized through an interrupte

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

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

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

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

206 l) piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate (Usmarapride, 12l).

207 ntermediates that spontaneously dehydrate to indazole oxides.

208 The indazole-paroxetine analogs were indeed more potent than

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

210 e high-yielding conversion of N2-derivatized indazoles (prepared from the corresponding 1H-indazoles)

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

212 lective, furnishing the alkylated indole and indazole products in a Markovnikov fashion with excellen

213 zole systems, including benzo[d]isothiazole, indazole, pyrazole and isoxazole.

214 y of amines (12 classes), including indoles, indazoles, pyrazoles, anilines, and sulfonamides.

215 converts in situ formed spiro[pyrazolo[1,2-a]indazole-pyrrolidine] into fused pyrazolopyrrolocinnolin

216 type addition to afford spiro[pyrazolo[1,2-a]indazole-pyrrolidine].

217 ed for the synthesis of spiro[pyrazolo[1,2-a]indazole-pyrrolidines] and fused pyrazolopyrrolo cinnoli

218 Indazoles represent a privileged scaffold in medicinal c

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

220 Nitrogen elimination from these (aza) indazoles results in the formation of (aza) fluorenes, f

221 nists can be replaced bioisosterically by an indazole, retaining the high GluN2B affinity and activit

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

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

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

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

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

227 without installing a protective group at the indazole ring using the ketone 6 as a common intermediat

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

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

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

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

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

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

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

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

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

237 We previously disclosed the discovery of an indazole series lead that demonstrated both safety and t

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

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

240 we describe the discovery of a "reinvented" indazole series with improved physicochemical properties

241 The synthesized indazoles showed very high GluN2B affinity but limited s

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

243 Several classes of azoles, including indazole, substituted pyrazole, benzotriazole, and tetra

244 Indazole substitution played a critical role in decreasi

245 tion yield and electron density at N2 of the indazole substrate, suggesting the importance of the ava

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

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

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

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

250 ogan cyclization at room temperature for 2 H-indazole synthesis.

251 functionalized annulated cyclic sulfonamide-indazoles that can be further converted into stable orga

252 e greater activity at the C-3 position of 1H-indazoles, the greater coordinating capacity of the N at

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

254 associated with scaffold progression from an indazole to 2-cyanoindole.

255 1 and 2 was replaced bioisosterically by an indazole to inhibit glucuronidation.

256 nt multidirectional syntheses of substituted indazoles to be realized.

257 ation of the photomediated transformation of indazoles to benzimidazoles through a nitrogen-carbon tr

258 described: route A by rearrangement of (aza) indazoles to diazo(aza)cyclohexadienes and (aza)cyclohex

259 ndazoles (prepared from the corresponding 1H-indazoles) to the corresponding benzimidazoles under UVB

260 rvous system (CNS)-penetrant 1-heteroaryl-1H-indazole type I (ATP competitive) LRRK2 inhibitors.

261 ioselective C3-H trifluoromethylation of 2 H-indazole under metal-free conditions, which proceeds via

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

263 tive allylation reaction of 1H-N-(benzoyloxy)indazoles using CuH catalysis.

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

265 proximal direct cyanation of N-aryl-(1H/2H)-indazoles via aerobic oxidative C(sp(2))-H bond activati

266 icient synthesis of functionalized 3-acyl-2H-indazoles via visible-light-induced self-catalyzed energ

267 nidation, its bioisosteric replacement by an indazole was envisaged.

268 -ortho-aroylation of substituted 1-phenyl-1H-indazole was obtained using dicumylperoxide (DCP) as the

269 e chemodivergent C-3 functionalization of 2H-indazoles was developed under aerobic conditions using c

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

271 A series of 3-aroyl indazoles was synthesized.

272 contrast to phenolic GluN2B antagonists, the indazoles were not conjugated with glucuronic acid.

273 Thiol-functionalized 2H-indazoles were synthesized under catalyst-, oxidant-, an

274 oved route was developed to form the desired indazole, which takes advantage of an electronically dir

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

276 tic method for C-3 alkoxycarbonylation of 2H-indazoles with carbazates under constant current in an u

277 The reaction of NH-indazoles with formaldehyde in aqueous hydrochloric acid

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

279 A variety of C3-allyl 1H-indazoles with quaternary stereocenters were efficiently

280 for the C3- and N-alkylation of indoles and indazoles with styrenes, catalyzed by Co complexes based

281 A number of 3-(phenylselanyl)-2H-indazoles with wide functional group tolerance have been

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

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

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

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

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

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

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

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