cas 27514-07-4, 7-Azabicyclo[2,2,1]heptane hydrochloride

Articles about 27514-07-4Total 12 be found

Unexpected resistance to base-catalyzed hydrolysis of nitrogen pyramidal amides based on the 7-azabicyclic[2.2.1]heptane scaffold
Non-planar amides are usually transitional structures, that are involved in amide bond rotation and inversion of the nitrogen atom, but some ground-minimum non-planar amides have been reported. Non-planar amides are generally sensitive to water or other n
De Velasco, Diego Antonio Ocampo Gutiérrez,Su, Aoze,Zhai, Luhan,Kinoshita, Satowa,Otani, Yuko,Ohwada, Tomohiko
(2018/09/26)

CENTRALLY ACTIVE AND ORALLY BIOAVAILABLE ANTIDOTES FOR ORGANOPHOSPHATE EXPOSURE AND METHODS FOR MAKING AND USING THEM
In alternative embodiments, the invention provides nucleophilic hydroxyimino- acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino- acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi- chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.
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Page/Page column 51

(2014/09/03)

7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands
A series of N-substituted 7-azabicyclo[2.2.1]heptanes (12-17 and 22-25) and similarly substituted pyrrolidines (32-36 and 41-44) were synthesized as sterically-reduced, achiral analogs of adamantane- and trishomocubane-derived σ ligands. In vitro competition binding assays against σ receptors revealed that arylalkyl N-substituents conferred selectivity for the σ2 subtype, while alicyclic or polycarbocyclic substituents imparted high affinity for both subtypes. The σ2 binding and subtype selectivities of N-arylalkyl-7-azanorbornanes was generally greater than the analogously-substituted pyrrolidines, indicating that steric bulk and conformational restriction around the nitrogen atom are likely important for subtype discrimination.
Banister, Samuel D.,Rendina, Louis M.,Kassiou, Michael
supporting information; experimental part
p. 4059 - 4063
(2012/07/03)

PROCESS FOR PREPARING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2. 1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A- HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.
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(2011/05/06)

PROCESSES FOR PRODUCING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).
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(2011/12/04)

SOLID FORMS OF N-(4-(7-AZABICYCLO[2.2.1]HEPTAN-7-YL)-2-TRIFLUOROMETHYL)PHENYL)-4-OXO-5-(TRIFLUOROMETHYL)-1,4-DIHYDROQUINOLINE-3-CARBOXAMIDE
The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.
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Page/Page column 41

(2011/05/06)

Fischer synthesis of isomeric thienopyrrole LHRH antagonists
As part of a structure-activity exploration into LHRH antagonists, structures containing the thieno[2,3-b]pyrrole core were identified as potent antagonists. This letter describes the employment of the Fischer synthesis to access this thienopyrrole and isomeric final compounds.
Andrews, David M.,Arnould, Jean-Claude,Boutron, Pascal,Délouvrie, Bénédicte,Delvare, Christian,Foote, Kevin M.,Hamon, Annie,Harris, Craig S.,Lambert-van der Brempt, Christine,Lamorlette, Maryannick,Matusiak, Zbegniew M.
experimental part
p. 5805 - 5816
(2009/12/24)

PYRROLE DERIVATIVES AS GONADOTROPIN RELEASING HORMONE (GNRH) ANTAGONISTS
The invention relates to a group of novel thieno-pyrrole compounds of formula (I) wherein: R1,R2, R3, R4 M, and R5 are as defined in the specification, as inter alia, gonadotrophin releasing hor
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(2008/06/13)

THIENOPYROLES AS ANTAGONISTS OF GNRH
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I) wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormon
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Page/Page column 65

(2010/02/13)

6H-THIENO`2, 3-B!PYRROLE DERIVATIVES AS ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE (GNRH)
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
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Page 88-89

(2008/06/13)

Synthesis of N-heteroaryl-7-azabicyclo[2.2.1]heptane derivatives via palladium-bisimidazol-2-ylidene complex catalyzed amination reactions
(equation presented) A one-step approach to novel N-heteroaryl-substituted-7-azabicyclo[2.2.1]heptanes from readily available heteroaryl halides and 7-azabicyclo-[2.2.1]heptane has been achieved. The cross-coupling amination reaction employs palladium-bis
Cheng, Jie,Trudell, Mark L.
p. 1371 - 1373
(2007/10/03)

The Nitrogen Inversion Barrier of 7-Methyl-7-azabicycloheptane and the "Bicyclic Effect"
The free energy of activation for nitrogen inversion of the title compound was determined to be 13.77(4) kcal/mol at 25 deg C in CDCl3 by dynamic (13)C NMR and that for the 7-ethyl compound to be 13.17(4) kcal/mol under the same conditions.The change in α(av) (the average of the three bond angles at nitrogen) during nitrogen inversion is used to assist comparison of inversion barriers for amines with different substituents attached.Comparison with literature data and AM1 calculations indicate that the barrier increase for 7-methyl-7-azabicycloheptane Ninversion relative to an α-unbranched monocyclic compound of the same pyramidality at nitrogen is on the order of 3.5 kcal/mol, while the less strained 1-bridge-azabicyclononyl and -octyl systems show barrier increases of about 1.5 kcal/mol.This represents an estimate of the size of Lehn's "bicyclic effect".
Nelsen, Stephen F.,Ippoliti, J. Thomas,Frigo, Timothy B.,Petillo, Peter A.
p. 1776 - 1781
(2007/10/02)