Tag: 200-300

On April 26, 2012, Connolly, Peter J.; Bian, Haiyan; Li, Xun; Liu, Li; Macielag, Mark J.; McDonnell, Mark E. published a patent.Application of 1251006-64-0 The title of the patent was Azetidinylpiperidine derivatives as monoacylglycerol lipase inhibitors and their preparation and use for the treatment of inflammatory pain. And the patent contained the following:

The invention relates to azetidinylpiperidine of formula I, which are monoacylglycerol lipase (MGL) inhibitors and which are useful in the treatment of inflammatory pain. Compounds of formula I wherein Y and Z are independently (un)substituted C6-10 aryl, (un)substituted thiazolyl, (un)substituted isothiazolyl, etc.; R is H and OH; with provisions; and enantiomers, diastereoisomers and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their MGL inhibitory activity. From the assay, it was determined that compound II exhibited an IC50 value of 0.006 μM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Application of 1251006-64-0

The Article related to azetidinyl piperidine preparation monoacylglycerol lipase inhibitor treatment inflammatory pain, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 1251006-64-0

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

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 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 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

Wang, Dongping; Mao, Jincheng; Zhu, Chen published an article in 2018, the title of the article was Visible light-promoted ring-opening functionalization of unstrained cycloalkanols via inert C-C bond scission.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

A novel, useful, visible light-promoted ring-opening functionalization of unstrained cycloalkanols was described. Upon scission of an inert cyclic C-C σ-bond, a set of medium- and large-sized rings were readily brominated under mild reaction conditions to afford the corresponding distal bromo-substituted alkyl ketones that were hard to synthesize otherwise. The products were versatile building blocks, which were easily converted to other valuable mols. in one-step operation. This protocol was also applicable to the unprecedented ring-opening cyanation and alkynylation of unstrained cycloalkanols. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to cycloalkanol iridium photocatalyst ring opening bromination, bromoalkyl ketone preparation, Aliphatic Compounds: Ketones and Derivatives, Including Sulfur Analogs and other aspects.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 7, 2018, Crew, Andrew P.; Qian, Yimin; Dong, Hanqing; Wang, Jing; Hornberger, Keith R.; Crews, Craig M. published a patent.Related Products of 1251006-64-0 The title of the patent was Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders and their preparation. And the patent contained the following:

The disclosure relates to bifunctional compounds of formulas I and II, which find utility as modulators of estrogen receptor (target protein). In particular, the disclosure is directed to bifunctional compounds of formula I and II, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, inhibitors of apoptosis proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the resp. E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Compounds of formula I and II wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds and E3 ubiquitin ligase; L is a bond and a chem. linking moiety; each X is independently CH and N; R1 is mono-, di- and trisubstitution and is independently OH, halo, alkoxy, MeO, EtO and acyloxy; R2 is mono- or disubstitution and is independently H, halo, CN, (un)branched alkyl, etc.; R3 is mono- or disubstitution and is independently H, and halo; R4 is H, alkyl, Me and Et; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs, and prodrugs thereof, are claimed. Example compound III was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen receptor degradation activity. From the assay, it was determined that compound III exhibited IC50 value of 0.35 nM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Related Products of 1251006-64-0

The Article related to tetrahydronaphthalene tetrahydroisoquinoline preparation estrogen receptor degrader, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Related Products of 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 10, 2015, Takayama, Tetsuo; Shibata, Tsuyoshi; Shiozawa, Fumiyasu; Kawabe, Kenichi; Shimizu, Yuki; Hamada, Makoto; Hiradate, Akira; Takahashi, Masato; Ushiyama, Fumihito; Oi, Takahiro; Shirasaki, Yoshihisa; Matsuda, Daisuke; Koizumi, Chie; Kato, Sota published a patent.Synthetic Route of 362703-57-9 The title of the patent was Pharmaceutical compositions containing N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine as prolyl hydroxylase 2 (PHD2) inhibitor. And the patent contained the following:

Oral solid pharmaceutical compositions contain N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine or its pharmaceutically acceptable salt as active ingredient. The compound inhibits PHD2, thus useful for prevention and treatment of anemia. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to tetrahydropyridinylcarbonylglycine preparation antianemic prolyl hydroxylase inhibitor oral solid, Pharmacology: Effects Of Cardiovascular, Hematologic, and Renal Drugs and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On November 24, 2021, Dorsheimer, Julia R.; Ashley, Melissa A.; Rovis, Tomislav published an article.Synthetic Route of 362703-57-9 The title of the article was Dual Nickel/Photoredox-Catalyzed Deaminative Cross-Coupling of Sterically Hindered Primary Amines. And the article contained the following:

Authors report a method to activate α-3° amines for deaminative arylation via condensation with an electron-rich aldehyde and merge this reactivity with nickel metallaphotoredox to generate benzylic quaternary centers, a common motif in pharmaceuticals and natural products. The reaction is accelerated by added ammonium salts. Evidence is provided in support of two roles for the additive – inhibition of nickel black formation and acceleration of the overall reaction rate. Authors demonstrate a robust scope of amine and haloarene coupling partners and show an expedited synthesis of ALK2 inhibitors. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to primary amine deaminative cross coupling nickel photoredox, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: General and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 28, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Qian, Yimin; Crews, Craig M.; Jaime-Figueroa, Saul published a patent.COA of Formula: C13H24N2O2 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, such as c-RAF, A-RAF and/or B-RAF, the target protein). In particular, the present disclosure is directed to bifunctional compounds 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, 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. Thus, 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).COA of Formula: C13H24N2O2

The Article related to dipeptide preparation apoptosis fibrosarcoma polypeptide modulator ubiquitin ligase, heterocycle preparation braf protein target degradation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.COA of Formula: C13H24N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem