cas 171049-35-7, N-BOC-4,4'-BIPIPERIDINE | Articles data

Articles about 171049-35-7Total 11 be found

Article title
Article abstract
Author
Journal number and time
Download

Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease
Herein, we describe the development of a functionally selective liver X receptor β (LXRβ) agonist series optimized for Emax selectivity, solubility, and physical properties to allow efficacy and safety studies in vivo. Compound 9 showed central pharmacodynamic effects in rodent models, evidenced by statistically significant increases in apolipoprotein E (apoE) and ATP-binding cassette transporter levels in the brain, along with a greatly improved peripheral lipid safety profile when compared to those of full dual agonists. These findings were replicated by subchronic dosing studies in non-human primates, where cerebrospinal fluid levels of apoE and amyloid-β peptides were increased concomitantly with an improved peripheral lipid profile relative to that of nonselective compounds. These results suggest that optimization of LXR agonists for Emax selectivity may have the potential to circumvent the adverse lipid-related effects of hepatic LXR activity.
Stachel, Shawn J.,Zerbinatti, Celina,Rudd, Michael T.,Cosden, Mali,Suon, Sokreine,Nanda, Kausik K.,Wessner, Keith,Dimuzio, Jillian,Maxwell, Jill,Wu, Zhenhua,Uslaner, Jason M.,Michener, Maria S.,Szczerba, Peter,Brnardic, Edward,Rada, Vanessa,Kim, Yuntae,Meissner, Robert,Wuelfing, Peter,Yuan, Yang,Ballard, Jeanine,Holahan, Marie,Klein, Daniel J.,Lu, Jun,Fradera, Xavier,Parthasarathy, Gopal,Uebele, Victor N.,Chen, Zhongguo,Li, Yingjie,Li, Jian,Cooke, Andrew J.,Bennett, D. Jonathan,Bilodeau, Mark T.,Renger, John
p. 3489 - 3498
(2016)
Read Online

BISPIPERIDINYL DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE
In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, Q and R5/s
-
Page/Page column 43; 44

(2017/05/28)

2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER
Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
-
Page/Page column 144

(2009/04/25)

[35S]GTPγS binding studies of amphiphilic drugs-activated Gi proteins: A caveat
This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [35S]GTPγS to different subtypes of Gi protein. The problem arose from the strong affinity between [35S]GTPγS and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results.
Manetti, Dina,Mannelli, Lorenzo Di Cesare,Dei, Silvia,Guandalini, Luca,Martini, Elisabetta,Banchelli, Martina,Ghelardini, Carla
scheme or table
p. 2224 - 2229
(2009/12/07)

Imidazopyridine Kinase Inhibitors
The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
-
Page/Page column 105

(2009/01/20)

Benzenesulphonamide derivatives, method for production and use thereof for treatment of pain
The present invention concerns novel benzenesulphonamide compounds, defined by formula I and the description, their method of preparation and their use in therapy.
-
Page/Page column 17

(2008/06/13)

Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate Gi proteins
Heterotrimeric G proteins play a pivotal role in the communication of cells with the environment. G proteins are stimulated by cell surface receptors (GPCR) that catalyze the exchange of GDP, bound to Gα subunit, with GTP and can per se be the target of drugs. Based on the structure of two nonpeptidic modulators of Gi proteins, a series of new molecules characterized by a long hydrophobic chain and at least two nitrogen atoms protonated at physiological pH was designed. The compounds were tested for their ability to stimulate binding of GTPγS to recombinant Gi proteins. Gi activation properties were also evaluated by inhibition of adenylyl cyclase activity in intact lymphocytes. Most compounds were able to stimulate GTPγS binding and to inhibit cAMP production at micromolar doses. Among the active compounds, 34 showed good efficacy and was the most potent compound studied, particularly on αo subtype; its regioisomer, 36, was the most efficacious one. Compound 7 showed also an interesting profile as it showed selectivity toward the αo subtype, in both efficacy and potency. Some of the compounds synthesized and found to be active may be useful leads to develop more potent and selective Gi protein modulators.
Manetti, Dina,Mannelli, Lorenzo Di Cesare,Dei, Silvia,Galeotti, Nicoletta,Ghelardini, Carla,Romanelli, Maria Novella,Scapecchi, Serena,Teodori, Elisabetta,Pacini, Alessandra,Bartolini, Alessandro,Gualtieri, Fulvio
p. 6491 - 6503
(2007/10/03)

17 Beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of
-
Page 21

(2008/06/13)

Bicyclic fibrinogen antagonists
This invention relates to compounds of the formulae: wherein A1is O, S, N—R1or CHR1; A4is N—R4or CHR4; R2is a sidechain containing an acid or ester group; R1, R4and R5are substituents such as H, alkyl and aryl alkyl, and R6is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
-
(2008/06/13)

Design, synthesis, and biological activity of methoctramine-related polyamines as putative Gi protein activators
The universal template approach provided a prospect of modifying methoctramine (2) structure. Thus, polyamines 3-7 were designed in which the flexibility of the diaminohexane spacer of 2 was replaced by a bipiperidinyl moiety. In electrically stimulated g
Melchiorre,Bolognesi,Budriesi,Ghelardini,Chiarini,Minarini,Rosini,Tumiatti,Wade
p. 4035 - 4038
(2007/10/03)

Integrin receptor antagonists
Compounds of formula (I) STR1 wherein A1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R3 or R4 ; X1 --X2 is CHR1 --CH, CR1 =CH, NR1 --CH, S(O)u --CH or O--CH; X3 is CR5 R5 ', NR5, S(O)u or O; R2 is --OR', --NR'R", --NR'SO2 R'", --NR'OR', --OCR'2 C(O)OR', --OCR'2 OC(O)--R', --OCR'2 C(O)NR'2, CF3 or --COCR'2 R2 '; R3, R4 and R7 are independently H, halo, --OR12, --SR12, --CN, --NR'R12, --NO2, --CF3, CF3 S(O)r --, --CO2 R', --CONR'2, R14 --C0-6 alky-, R14 --C1-6 oxoalkyl-, R14 --C2-6 alkenyl-, R14 --C2-6 alkynyl-, R14 --C0-6 alkyloxy-, R14 --C0-6 alkylamino- or R14 --C0-6 alkyl--S(O)r --; R6 is W--(CR'2)q --Z--(CR'R10)--U--(CR'2)s --V-- or W'--(CR'2)q --U--(CR'2)s -- U and V are absent or CO, CR'2, C(=CR152), S(O)n, O, NR15, CR15 'OR15, CR'(OR")CR'2, CR'2 CR'(OR") C(O)CR'2, CR152 C(O), CONR15, NR15 CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR15, NR15 C(S), SO2 NR15, NR15 SO2, N=N, NR15 NR15, NR15 CR152, NR15 CR152, CR152 O, OCR152, C$(m)ZC, CR15 =CR15, Het, or Ar, provided that U and V are not simultaneously absent, and W and W' are a nitrogen-containing substituent, and integrin receptor antagonists.
-
(2008/06/13)