ライフサイエンスコーパス: piperidinyl

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1 sist of the piperidine analogues N1,N3-bis(4-piperidinyl)-1,3-diaminopropane, N1,N4-bis(4-piperidinyl

2 piperidinyl)-1,3-diaminopropane, N1,N4-bis(4-piperidinyl)-1,4-diaminobutane, N1,N4-bis(4-piperidinylm

3 Thalidomide, 2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione, has been shown

4 (1-methylcyclooctyl)-4-piperidinyl]-2-(3R)-3-piperidinyl-1H-benzimidazole trihydrochloride] and NNC 6

5 ichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyr azole-3-carboxamide] (30 microg in 50

6 ichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazo le-3-carboxamide (AM251), had a si

7 ichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3 -carboxamide] blocked these re

8 ichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3- carboxamide (AM251) was coapp

9 ichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-ca rboxamide (AM251) through d

10 N-(1-Benzyl-4-piperidinyl)-2,4-dichlorobenzamide 5 (BPDBA) is a noncom

11 A series of N-(4-piperidinyl)-2-indolinones were discovered as a new stru

12 ipid transport, 2-[1-(3, 3-diphenylpropyl)-4-piperidinyl]-2,3-dihydro-1H-isoindol-1-o ne (BMS-200150)

13 ligands MCOPPB [1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-(3R)-3-piperidinyl-1H-benzimidazole trihy

14 ex = 294), and 5-amino-3-[4-(p-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4,-tetrahydronaphthale ne (

15 dex = 70), trans-3-[4-(5-iodothienylcarbonyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphth alene (2

16 mpounds, namely, trans-3-[4-(4-fluorobenzoyl)piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (28

17 inyl]amino}-3,5- dimethyl-1H-pyrazol-1-yl)-1-piperidinyl]-2-hydroxy-1-propanone (AZD9362, 28), a nove

18 enzo[5, 6]cyclohepta[1, 2-b]pyridin-11-yl)-1-piperidinyl]-2-oxoethyl]-1-piperidinecarbo xamide ).

19 5, 6]cyclohepta[1, 2-b]pyridin-11-ylidene)-1-piperidinyl]-2-oxoethyl]pyridine N-oxide where DeltaH de

20 2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile) and IKK 16 prevente

21 R*)-1-(cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl -1,3-dihydro-2H-benzimidazol-2-one]

22 s, N-(3-{1-[4-(3,4-difluorophenoxy)benzyl]-4-piperidinyl}-4-methylphenyl)-2-methylpr opanamide (16g,

23 5,7-dihydroxyphenyl-8-[4-(3-hydroxy-1-methyl)piperidinyl] -4H-1-benzopyran-4-one hydrochloride hemihy

24 nding of the CB1-selective antagonist [3H]N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4

25 reatment study using the CB(1) antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4

26 Analogues of the biaryl pyrazole N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4

27 -N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-iodo-2- methoxybenzamide (123I-5-I-R91150

28 ompound, RWJ-37868, 2-(4-chlorobenzoyl)-4-(1-piperidinyl-acetyl)-1,3,5-trimethylpyrrole++ + (4d), sho

29 three of the 5-[[4-[(4-dialkylamino)butyl]-1-piperidinyl]acetyl]-10, 11-dihydro-5-H-dibenzo[b,e][1,4]

30 2-dimethyl-1-oxopentyl)ethylamino]pro pyl]-1-piperidinyl]acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6

31 2-dimethyl-1-oxopentyl)ethylamino]prop yl]-1-piperidinyl]acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6

32 H(CH3)2), and either the pyrrolidinyl or the piperidinyl analogues.

33 ith NH2, N-alkyl, N,N-dialkyl, pyrrolidinyl, piperidinyl, and piperazinyl substituents at the 2-posit

34 Resultantly, two piperidinyl- and two quinuclidinium-substituted biphenyl

35 ceptor (NK(2)R) binding of [(3)H]-SR48968, a piperidinyl antagonist, is inhibited by methanethiosulfo

36 ecule antagonists of CCR4, featuring a novel piperidinyl-azetidine motif, that inhibit the recruitmen

37 A PARP inhibitor, 3, 4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone (DPQ; IC50=1 mi

38 with the PARP inhibitor 3,4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone both showed inc

39 by >80% either by 10 muM 3,4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone, an established

40 ia by the PARP inhibitor 3,4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2h)-isoquinolinone.

41 PARP enzymatic inhibitor 3,4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2h)-isoquinolinone.

42 by the PARP-1 inhibitor 3,4-dihydro-5-[4-(1-piperidinyl)butoxyl]-1(2H)-isoquinolinone (DPQ), whilst

43 hyl-7-chloro-6,7,8-trideoxy-6-[[(4-undecyl-2-piperidinyl)carbonyl]amino ]-1-thiomonohydrochloride (2S

44 , N-[4-[[1-[2-(6-methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesul fonamide, 2HCl (E

45 ed a p-iodophenyl group at the 5-position, a piperidinyl carboxamide at the 3-position, and a 2,4-dic

46 Both compounds possess a piperidinyl crotonamide Michael acceptor and a 3-chloro-

47 uncated analogues of our previously reported piperidinyl derivatives (3).

48 monovalent fragments biphenyl carbamic acid piperidinyl ester (MA) and BA, respectively.

49 nyl group with oxygen ([6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]b enzo[b

50 (S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H- 1-benzopyran-7-ol (EM652)

51 henyl)-6-hydroxybenzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride (2), i

52 Arzoxifene ([6-hydroxy-3-[4-[2-(1-piperidinyl)-ethoxy]phenoxy]-2-(4-methoxyphenyl)]be nzo[

53 (3-hydroxyphenyl)sulfonyl]-2 -(2-(4-methyl-1-piperidinyl)ethyl)pyrrolidine (SB-269970) mimicked the e

54 ethyl)-1,4-diaminobutane, and N1,N4-bis[2-(4-piperidinyl)ethyl]-1,4-diaminobutane and the pyridine an

55 d 3-[2-[4-(bis-(4-fluorophenyl) methylene]-1-piperidinyl)ethyl]-2,3-dihydro-2-thioxo-4(1H)quinazolino

56 Radioiodinated benzamide N-[2-(1'-piperidinyl)ethyl]-3-[125I]iodo-4-methoxybenzamide ([125

57 nzamides, [125I]PIMBA, 4-[125I]iodo-N-[2-(1'-piperidinyl)ethyl]benzamide, and 2-[125I]-N-(N-benzylpip

58 f one congener member (4-[125I]iodo-N-[2-(1'-piperidinyl)ethyl]benzenesulfonamide, 4-[125I]IPBS) was

59 yclo[3.3.1.1(3, 7)]dec-1-ylcarbonyl)amino]-1-piperidinyl]ethyl]-1H-indazole-3- carboxamide) as a pote

60 nist ketanserin (3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedion e tartrate

61 brorphine, isotonitazene, metonitazene, or N-piperidinyl etonitazene).

62 phine, isotonitazene, metonitazene, and/or N-piperidinyl etonitazene.

63 rphine, isotonitazene, metonitazene and/or N-piperidinyl etonitazene.

64 in the (3R,4R)-3,4-dimethyl-4-(hydroxyphenyl)piperidinyl group represents the message, and the basic

65 (EC(50) = 90 nM) bearing a dimethylamino or piperidinyl group, respectively, at position 4 of the ph

66 pyridinyl, piperazinyl, homopiperazinyl, and piperidinyl groups were synthesized.

67 imide (NEM), N-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl)-iodacetamide (IASL), N-[[(iodoacetyl)amino]

68 ntified (2-(4-methoxyphenyl)-4-quinolinyl)(2-piperidinyl)methanol (5) (NSC23925) to be a small molecu

69 )methyl]-1H-indazole-3-carboxamide and 4-[(4-piperidinyl)methoxy]-2H-pyrrolo[3,4-c]quinoline derivati

70 -[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl}-(2-methylbutyl]-1,2,3,4-tetrahydro-

71 -[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl}-(2-methylpropyl]-2-methyl-1,2,3,4-t

72 {[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-

73 {[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl ]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-

74 his study we describe the discovery of N-[(4-piperidinyl)methyl]-1H-indazole-3-carboxamide and 4-[(4-

75 (3 R,4 R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4 -tetrahydro-

76 e-activity relationship optimization, a 3-(N-piperidinyl)methylbenzamide derivative 13d markedly prot

77 gnificantly enhanced by incorporation of a 4-piperidinyl moiety at the 2-position of the imidazole wh

78 inetic estimates (k(3)) of 1-[(11)C]methyl-4-piperidinyl n-butyrate ([(11)C]BMP) hydrolysis determine

79 group of the methyl ester is H-bonded to the piperidinyl N-H may be the bioactive form of the molecul

80 talyst system (TEMPO = 2,2,6,6-tetramethyl-1-piperidinyl-N-oxyl) displays excellent chemo- and regios

81 t (Pyrene-TEMPO (TEMPO = 2,2,6,6-tetramethyl piperidinyl-N-oxyl)) immobilized on the surface of modif

82 electron donors 4-(N-pyrrolidinyl)- and 4-(N-piperidinyl)naphthalene-1,8-dicarboximide, 5ANI and 6ANI

83 where MeOAn = p-methoxyaniline, 6ANI = 4-(N-piperidinyl)naphthalene-1,8-dicarboximide, and NI = naph

84 where MeOAn = p-methoxyaniline, 6ANI = 4-(N-piperidinyl)naphthalene-1,8-dicarboximide, Ph = phenyl,

85 zyl)benzamides (2, 3a-e), N, N-diethyl(alpha-piperidinyl or piperidinylidenebenzyl)benzamides (4a, 5a

86 trifluoroethyl groups and incorporation into piperidinyl or pyridyl systems.

87 oromethylenated spiro-pyrrolidinyl and spiro-piperidinyl oxindoles is described.

88 oromethylenated spiro-pyrrolidinyl and spiro-piperidinyl oxindoles.

89 beta-methyl-5-(3-hydroxyphenyl)-7alpha-[3-(1-piperidinyl)p ropanamido]morphan [(-)-3b] was identified

90 enyl-N-[1-(2-(4-isothiocyanato)-phenethyl)-4-piperidinyl]-p ropana mide-HCl (delta-selective) to exam

91 ylpropyl)-2-aza bicyclo[3.3.1]non-7-yl]-3-(1-piperidinyl)propanamide (5a, KAA-1) as the first potent

92 ne-1,3-diol (8) and 2-(2,2,6,6-tetramethyl-1-piperidinyl)propane-1,3-diol (10) may be prepared easily

93 y hindered dimethyl 2-(2,2,6,6-tetramethyl-1-piperidinyl)propanedioate was formed in 38% yield from 2

94 ructural MRI, PET scanning with 11C-methyl-4-piperidinyl propionate (PMP) as a measure of cortical ac

95 rwent a clinical assessment, [(11)C]methyl-4-piperidinyl propionate acetylcholinesterase brain positr

96 azepine channel inhibitor 4-[-3{1-(4-benzyl) piperidinyl}propionyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-

97 The 3-(3-piperidinyl)propyl in 33 was found to maximize affinity

98 eridine HCl) and 77-LH-28-1 (1-(3-(4-butyl-1-piperidinyl)propyl)- 3,3-dihydro-2(1H)-quinolinone).

99 structurally related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1, PD8

100 y investigates the efficacy of Compound 2, a piperidinyl pyrazolopyridine allosteric activator that b

101 , defluorinative halide exchange leaving the piperidinyl ring intact prevails when 4-fluoro- and 4,4-

102 o-dig radical cyclization to forge the final piperidinyl ring system.

103 chimeric nAChRs by bis(2,2,6,6-tetramethyl-4-piperidinyl) sebacate (bis-TMP-10 or BTMPS), a bifunctio

104 ible antagonists, bis-(2,2,6,6-tetramethyl-4-piperidinyl) sebacate (BTMPS), 2,2,6,6-tetramethylpiperi

105 The 4-piperazinyl- and 4-piperidinyl-substituted 3,4-dihydro-1(1H)-isoquinolinone