Day: November 1, 2022

On June 28, 2018, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Qian, Yimin; Crews, Craig M.; Jaime-Figueroa, Saul published a patent.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of heterocyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. And the patent contained the following:

The disclosure relates to bifunctional compounds of formula I, which find utility as modulators of rapidly accelerated fibrosarcoma (RAF, the target protein). The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the disclosure. Bifunctional compounds of formula I wherein ULM is a small mol. E3 ubiquitin ligand binding moiety that binds to E3 ubiquitin ligase selected from a group consisting of Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins or mouse double-minute homolog 2 ligand; PTM is a small mol. that binds the target protein RAF; L is a bond and a chem. linking moiety; and their pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their B-RAF degradation activity. From the assay, it was determined that compound II exhibited DC50 value in the range of < 100 nM to > 50 nM and Dmax value of > 70 %. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to heterocycle preparation braf protein target degradation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

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 September 2, 2021, Mellstedt, Haakan; Bystroem, Styrbjoern; Vaagberg, Jan; Olsson, Elisabeth published a patent.Quality Control of 1-Ethylpiperidin-4-amine dihydrochloride The title of the patent was 2-Phenylimidazo[4,5-B]pyridin-7-amine derivatives used as inhibitors of mammalian tyrosine kinase ROR1 activity and their preparation. And the patent contained the following:

The invention provides compounds of formula I and II and their use as inhibitors of mammalian tyrosine kinase ROR1. Compounds of formula I and II, wherein R1 is C1-6 alkyl, C3-6 cycloalkyl-C1-6 alkyl, cyano-C1-6 alkyl, etc.; Ra is independently C1-6 alkyl; x is 0, 1, 2, 3 and 4; m is 1 and 2; R2 is Cl and Br; Rb is halo, C1-3 alkyl and C1-3 alkoxy; y is 0, 1, 2 and 3; W is QR4, O and N(R5)CO; Q is N and CH; R4 is C1-6 alkyl, cyano-C1-6 alkyl, C1-6 alkyl-SO2, etc.; Z is N and CH; R3 is independently C1-6 alkyl; p is 0, 1, 2 and 3; n is 0, 1 and 2; and pharmaceutically acceptable salt thereof, are claimed. Compound III was prepared by a multistep procedure (procedure given). Compounds were tested for mammalian tyrosine kinase ROR1 inhibitory activity (data given). The experimental process involved the reaction of 1-Ethylpiperidin-4-amine dihydrochloride(cas: 357935-97-8).Quality Control of 1-Ethylpiperidin-4-amine dihydrochloride

The Article related to imidazole pyridine derivative preparation ror1 inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Quality Control of 1-Ethylpiperidin-4-amine dihydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 18, 2018, Mellstedt, Haakan; Bystroem, Styrbjoern; Vaagberg, Jan; Olsson, Elisabeth published a patent.Related Products of 357935-97-8 The title of the patent was 2-Phenylimidazo[4,5-B]pyridin-7-amine derivatives used as inhibitors of mammalian tyrosine kinase ROR1 activity and their preparation. And the patent contained the following:

The invention provides compounds of formula I and II and their use as inhibitors of mammalian tyrosine kinase ROR1. Compounds of formula I and II, wherein R1 is C1-6 alkyl, C3-6 cycloalkyl-C1-6 alkyl, cyano-C1-6 alkyl, etc.; Ra is independently C1-6 alkyl; x is 0, 1, 2, 3 and 4; m is 1 and 2; R2 is Cl and Br; Rb is halo, C1-3 alkyl and C1-3 alkoxy; y is 0, 1, 2 and 3; W is QR4, O and N(R5)CO; Q is N and CH; R4 is C1-6 alkyl, cyano-C1-6 alkyl, C1-6 alkyl-SO2, etc.; Z is N and CH; R3 is independently C1-6 alkyl; p is 0, 1, 2 and 3; n is 0, 1 and 2; and pharmaceutically acceptable salt thereof, are claimed. Compound III was prepared by a multistep procedure (procedure given). Compounds were tested for mammalian tyrosine kinase ROR1 inhibitory activity (data given). The experimental process involved the reaction of 1-Ethylpiperidin-4-amine dihydrochloride(cas: 357935-97-8).Related Products of 357935-97-8

The Article related to imidazole pyridine derivative preparation ror1 inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 357935-97-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 1, 2019, Crews, Craig M.; Burslem, George; Cromm, Philipp M.; Jaime-Figueroa, Saul; Toure, Momar published a patent.Category: piperidines The title of the patent was Preparation of imide-based compounds as modulators of proteolysis and methods of use. And the patent contained the following:

The description relates to imide-based compounds of formula I, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacol. activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type. Compounds of formula I wherein L is a chem. linker: PTM is a protein target moiety that binds to at target protein or polypeptide; CLM is a cereblon E3 ubiquitin ligase binding moiety; and salts, solvates, polymorphs, and deuterated forms thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their protein degradation activity (data given). The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Category: piperidines

The Article related to imide preparation protein degradation proteolysis modulator, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On February 9, 2017, Bradner, James; Buckley, Dennis; Winter, Georg published a patent.Formula: C14H10N2O6 The title of the patent was Methods to induce targeted protein degradation through bifunctional molecules. And the patent contained the following:

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to nucleic acids, polypeptides, cells, and methods for highly regulated, targeted degradation of proteins through the use of the bifunctional compounds A polynucleotide comprising a first nucleotide sequence encoding a first polypeptide to which a Targeting Ligand of formula I (wherein ring containing T1-T5 is (a) T1, T2, T4 = N; T3, T5 = C, or (b) T1 = N, T2 = O; T3-T5 = C; A1 is S and C=C; A2 is NH and derivatives and O; each R1 is independently C1-3 alkyl, (CH2)0-3CN, (CH2)0-3OH, etc.; R2 is H, C1-6 alkyl, (CH2)0-3heterocyclyl, etc.; R3 is independently C1-3 alkyl, (CH2)0-3CN, (CH2)0-3OH, etc.; R4 is C1-3 alkyl) is capable of binding, and a second nucleotide sequence encoding a second polypeptide, wherein the first polypeptide and the second polypeptide are linked together with a peptide bond to form a fused polypeptide, is claimed. Example compound II was prepared by acylation of N-(4-aminobutyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide trifluoroacetate with (S)-2-(4-(4-cyanophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetic acid. Exemplified compounds I demonstrated to have potent biol. activities, e.g., binding to the protein target, mediating protein degradation, etc. (data given). The title bifunctional compounds Degron-Linker-Targeting Ligand [Degron = I (ring A = II, III; Y = a bond, O, NH, etc.; X = C(O), C(R3); X1-X2 = C(R3):N or C(R3)2C(R3)2; R1 = halo, NO2, NH2, etc.; R3 = H, alkyl optionally substituted with aryl or 5-10 membered heteroaryl; each R31 = (independently) alkyl; R4 = (independently) H or alkyl; or two R4, together with the carbon atom to which they are attached, form C(O), carbocycle, or 4-6 membered heterocycle comprising 1-2 heteroatoms selected from N and O; R5 = H, alkyl, F or Cl; n = 0-2; m = 0-3; t = 0-1); Linker = IV (p1 = 0-12; p2 = 0-12; p3 = 0-6; each W = (independently) absent, CH2, O, S, NH or NR5; Z = absent, CH2, O, NH or NR5; each R5 = (independently) alkyl; Q = absent, C(O)NH, C(O)O, etc.); Targeting Ligand = V (ring containing T1-T5 = (a) T1, T2, T4 = N; T3, T5 = C, or (b) T1 = N, T2 = O; T3-T5 = C; A1 = S or C:C; A2 = NR15 or O; nn1 = 0-2; each R11 = (independently) alkyl, (CH2)0-3CN, (CH2)0-3halogen, etc.; R12 = H, alkyl, (CH2)0-3heterocyclyl, etc.; nn2 = 0-3; each R13 = alkyl, (CH2)0-3CN, (CH2)0-3halogen, etc.; R14 = alkyl; R15 = H or alkyl); with the proviso] which act as protein degradation inducing moieties, were prepared E.g., a multi-step synthesis of VI, starting from JQ1 (VII), was described. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the title bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. Exemplified compounds I demonstrated to have potent biol. activities, e.g., binding to the protein target (e.g. BRD4), mediating protein degradation, etc. (data given). The present application also provides methods for making compounds of the application and intermediates thereof. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Formula: C14H10N2O6

The Article related to bifunctional compound preparation targeted protein degradation inducer, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Formula: C14H10N2O6

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

Sriramudu, B.; Satyanarayana, B.; Rao, S. Venkat; Krishna, N.; Murali, Krishna P.; Ramachandran, D. published an article in 2018, the title of the article was Synthesis and characterization of biological active compounds contain benzimidazole piperidine analogues.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

A series of compounds namely, 1-(3-(piperidin-1-yl)propyl)-1H-benzo[d]imidazol-2(3H)-ones were synthesized from 1-(3-chloropropyl)-1H-benzo[d]imidazol-2(3H)-one and 4-substituted piperidines by using preamble chem. reactions, which exhibited good antibacterial and antifungal activities. They were structurally related to Domperidone, these results could help full for deriving more potential drug mols. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to chloropropyl benzimidazolone piperidine alkylation, piperidylpropyl benzimidazolone preparation antibacterial antifungal activity, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem