Category: 883984-95-0

On November 15, 2009, Burgey, Christopher S.; Potteiger, Craig M.; Deng, James Z.; Mosser, Scott D.; Salvatore, Christopher A.; Yu, Sean; Roller, Shane; Kane, Stefanie A.; Vacca, Joseph P.; Williams, Theresa M. published an article.Formula: C19H18ClN3O4 The title of the article was Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: Development of novel spiropiperidines. And the article contained the following:

Several novel spiropiperidine-based CGRP receptor antagonists have been developed that maintain good potency and have reduced potential for metabolism The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Formula: C19H18ClN3O4

The Article related to spiropiperidine cgrp receptor antagonist preparation migraine, Pharmacology: Structure-Activity and other aspects.Formula: C19H18ClN3O4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 2016, Fournier, Jean-Francois; Clary, Laurence; Thoreau, Etienne published a patent.COA of Formula: C19H18ClN3O4 The title of the patent was Preparation of heterocyclic compounds as GCRP receptor antagonist and their use in medicine and in cosmetics. And the patent contained the following:

The invention relates to heterocyclic compounds of formula I and their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to their use as drug, preferentially in the prevention and/or the treatment of inflammatory diseases with a component neurogene or their use as cosmetic. The compounds of this invention act like antagonists of receiver CGRP-R. Compounds of formula I wherein Y is CH2, CO, C(CH3)2 and spirocyclopropyl; R1 is (un)substituted piperidinyl, azabicyclyl, azaspirocyclyl, etc.; R2, R3 and R6 are independently H, F and Me; R4 is H, alkyl, alkenyl, alkynyl, etc.; R5 is halo, alkyl, cycloalkyl, (un)substituted Ph, etc.; and pharmaceutically acceptable salts and enantiomers thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their GCRP receptor antagonistic activity. From the assay, it was determined that compound II exhibited Kdapp in the range of 10 nM – 100 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).COA of Formula: C19H18ClN3O4

The Article related to heterocyclyl preparation gcrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.COA of Formula: C19H18ClN3O4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 24, 2016, Fournier, Jean-Francois; Clary, Laurence; Thoreau, Etienne published a patent.Quality Control of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of heterocyclic compounds as GCRP receptor antagonist and their use in medicine and in cosmetics. And the patent contained the following:

The invention relates to heterocyclic compounds of formula I and their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to their use as drug, preferentially in the prevention and/or the treatment of inflammatory diseases with a component neurogene or their use as cosmetic. The compounds of this invention act like antagonists of receiver CGRP-R. Compounds of formula I wherein Y is CH2, CO, C(CH3)2 and spirocyclopropyl; R1 is (un)substituted piperidinyl, azabicyclyl, azaspirocyclyl, etc.; R2, R3 and R6 are independently H, F and Me; R4 is H, alkyl, alkenyl, alkynyl, etc.; R5 is halo, alkyl, cycloalkyl, (un)substituted Ph, etc.; and pharmaceutically acceptable salts and enantiomers thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their GCRP receptor antagonistic activity. From the assay, it was determined that compound II exhibited Kdapp in the range of 10 nM – 100 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Quality Control of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to heterocyclyl preparation gcrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Quality Control of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 24, 2011, Williams, Theresa M. published a patent.HPLC of Formula: 883984-95-0 The title of the patent was Heterocyclic benzodiazepine cgrp receptor antagonists. And the patent contained the following:

Compounds of formula I:(where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).HPLC of Formula: 883984-95-0

The Article related to preparation benzodiazepine piperidine benzene, cgrp receptor antagonist treatment human headache migraine, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.HPLC of Formula: 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On February 8, 2007, Williams, Theresa M. published a patent.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of heterocyclic benzodiazepine derivatives as CGRP receptor antagonists. And the patent contained the following:

The title compounds with general formula I [wherein R2 = independently H, alkyl, cycloalkyl, aryl, heteroaryl, etc.; R7 = (un)substituted alkyl, alkenyl, alkynyl cycloalkyl, etc; D = N or C(R1), where R1 = independently (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, etc.; W = O, (un)substituted NH, or (un)substituted CH2; X = C or S; Y = O, N(CN), NC(=O)NH2, etc.; and Z = (un)substituted piperidinyl, aryl, or arylamino] or pharmaceutically acceptable salts and diastereomers thereof were prepared as antagonists of calcitonin gene-related peptide (CGRP) receptors for the treatment or prevention of diseases in which the CGRP is involved, such as migraine. For example, compound II was prepared in a multi-step synthesis. I showed antagonistic activity against CGRP receptor with IC50 values of about 50 μM in native receptor binding assay, native receptor functional assay, etc. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to preparation benzodiazepine piperidine benzene, cgrp receptor antagonist treatment human headache migraine, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Recommanded Product: Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 23, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of 4-aminopyrimidines as CGRP antagonists. And the patent contained the following:

Title compounds I [R1 = spirocylic heterocycles with provisos; R2 = H, alkyl, etc.; R3 = aryl, heteroaryl, etc.; U = N, N-oxide, etc.; V = N, N-oxide, etc.; X = N, N-oxide, etc.; Y = N, C-R7; R7 = H, halo, alkyl] and their pharmaceutically acceptable salts and formulations were prepared For example, N-arylation of a piperidine II and chloropyrimidine III afforded claimedaminopyrimidine IV in 55% yield. In CGRP inhibition assays, 2-examples of compounds I exhibited Ki values of 6 and 27 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to aminopyrimidine preparation cgrp antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Synthetic Route of 883984-95-0 The title of the patent was Preparation of as 2-oxoindoles CGRP receptor antagonists. And the patent contained the following:

Title compounds I [R1 = 2-oxoindole with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylene, etc.; U = N, N-oxide, CR5; V = N, N-oxide, CR6; X = N, N-oxide, CR7; Y = N, CR6; R5 = H, hyalo, CN, etc.; R6 = H, alkyl, etc.; R7 = H, halo, CN. etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, coupling of chloropyrimide II and amine III afforded claimed oxoindole IV. In CGRP receptor antagonists assays, 4-examples of compounds I exhibited Ki values ranging from 15-535 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Synthetic Route of 883984-95-0

The Article related to oxoindole preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Synthetic Route of 883984-95-0 The title of the patent was Preparation of as pyridin-2-ones as CGRP receptor antagonists. And the patent contained the following:

Title compounds I and II [R1 = 2-oxoindoles with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylenen, etc.; R5 = H, alkyl, benzyl, etc.;] and their pharmaceutically acceptable salts and formulations were prepared For example, deprotection of methoxypyridine III afforded claimed pyridinone IV. In CGRP receptor antagonists assays, compounds I and II exhibited Ki values ≤50 μM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Synthetic Route of 883984-95-0

The Article related to pyridinone preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 5, 2012, Inoue, Yasunao; Konishi, Yasuko published a patent.HPLC of Formula: 883984-95-0 The title of the patent was Preparation of polycyclic spiro-piperidine derivatives as M1 and M4 agonists. And the patent contained the following:

Disclosed are compounds I [R1 = (un)substituted alkyl; R2-R4 = H, halo, (un)substituted alkyl, etc.; R5 = H, (un)substituted alkyl, (un)substituted cycloalkyl, etc.; R6, R7 = H or (un)substituted alkyl; R6 and R7, together with the carbon atom to which they are attached, may combine to form C:O group with a proviso that when Y is oxygen, R6 and R7, together with the carbon atom to which they are attached, may combine to form C:O group; m, n = 1-3; A = single bond or CH2; X = NH, oxygen or sulfur atom; Y = CR8R9 or oxygen atom; R8, R9 = H or alkyl; or pharmaceutically acceptable salts thereof], useful for the treatment of Alzheimer disease and schizophrenia. For example, compound II was prepared via reaction of N-tert-butoxycarbonylpiperidone with tri-Et phosphonoacetate followed by treatment with DBU, amidation with 2-amino-3-bromopyridine, Pd(OAc)2-catalyzed cyclization, dealkoxycarbonylation using HCl, and reaction with Et 4-formylpiperidine-1-carboxylate/NaBH(OAc)3. Compound II exhibited agonistic activities of 89%, 66%, 21%, and 138% (at 1 μM) for M1, M2, M3, and M4, resp. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).HPLC of Formula: 883984-95-0

The Article related to polycyclic spiro piperidine preparation m1 m4 agonist, alzheimer disease schizophrenia treatment polycyclic spiro piperidine, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.HPLC of Formula: 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 21, 2018, Mowrey, Dale R.; Reif, James J.; Milkiewicz, Karen L.; Allwein, Shawn P. published an article.Related Products of 883984-95-0 The title of the article was Development of a Novel Process for the Kilogram-Scale Synthesis of Spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one. And the article contained the following:

The dihydrochloride of spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one I·2 HCl was prepared on kilogram scale by base-mediated Boc protection of 3-bromo-2-pyridinamine, metalation with i-PrMgCl and spirocyclization with 1-Boc-4-piperidinone, and Boc deprotection with aqueous HCl in isopropanol. A two-batch kilo lab campaign generated I·2 HCl in >99% HPLC area purity and in 77% overall yield. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Related Products of 883984-95-0

The Article related to spiropyridooxazinepiperidinone kilogram scale preparation, butoxycarbonylation bromopyridinamine metalation spirocyclization butoxycarbonylpiperidone neutralization kilogram scale and other aspects.Related Products of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem