Category: 1251006-64-0

On March 12, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmerman, Kurt published a patent.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. And the patent contained the following:

The present disclosure relates to bifunctional compounds, ULM- L-PTM, 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, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present 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 present disclosure. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to polycyclic targeted protein kinase raf, Pharmaceuticals: Pharmaceutics and other aspects.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

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

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

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 August 13, 2020, Robles, Omar; Jackson, Jeffrey J.; Marshall, Lisa; Talay, Oezcan; Chian, David; Cutler, Gene; Diokno, Raymond; Hu, Dennis X.; Jacobson, Scott; Karbarz, Emily; Kassner, Paul D.; Ketcham, John M.; McKinnell, Jenny; Meleza, Cesar; Reilly, Maureen K.; Riegler, Erin; Shunatona, Hunter P.; Wadsworth, Angela; Younai, Ashkaan; Brockstedt, Dirk G.; Wustrow, David J.; Zibinsky, Mikhail published an article.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the article was Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors. And the article contained the following:

The C-C chemokine receptor 4 (CCR4) is broadly expressed on regulatory T cells (Treg) as well as other circulating and tissue-resident T cells. Treg can be recruited to the tumor microenvironment (TME) through the C-C chemokines CCL17 and CCL22. Treg accumulation in the TME has been shown to dampen the antitumor immune response and is thought to be an important driver in tumor immune evasion. Preclin. and clin. data suggest that reducing the Treg population in the TME can potentiate the antitumor immune response of checkpoint inhibitors. We have developed small-mol. antagonists of CCR4, featuring a novel piperidinyl-azetidine motif, that inhibit the recruitment of Treg into the TME and elicit antitumor responses as a single agent or in combination with an immune checkpoint blockade. The discovery of these potent, selective, and orally bioavailable CCR4 antagonists(I), and their activity in in vitro and in vivo models, is described herein. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to antitumor ccr4 antagonists checkpoint inhibitors combination immune response bioavailability, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

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

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 August 13, 2020, Robles, Omar; Jackson, Jeffrey J.; Marshall, Lisa; Talay, Oezcan; Chian, David; Cutler, Gene; Diokno, Raymond; Hu, Dennis X.; Jacobson, Scott; Karbarz, Emily; Kassner, Paul D.; Ketcham, John M.; McKinnell, Jenny; Meleza, Cesar; Reilly, Maureen K.; Riegler, Erin; Shunatona, Hunter P.; Wadsworth, Angela; Younai, Ashkaan; Brockstedt, Dirk G.; Wustrow, David J.; Zibinsky, Mikhail published an article.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the article was Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors. And the article contained the following:

The C-C chemokine receptor 4 (CCR4) is broadly expressed on regulatory T cells (Treg) as well as other circulating and tissue-resident T cells. Treg can be recruited to the tumor microenvironment (TME) through the C-C chemokines CCL17 and CCL22. Treg accumulation in the TME has been shown to dampen the antitumor immune response and is thought to be an important driver in tumor immune evasion. Preclin. and clin. data suggest that reducing the Treg population in the TME can potentiate the antitumor immune response of checkpoint inhibitors. We have developed small-mol. antagonists of CCR4, featuring a novel piperidinyl-azetidine motif, that inhibit the recruitment of Treg into the TME and elicit antitumor responses as a single agent or in combination with an immune checkpoint blockade. The discovery of these potent, selective, and orally bioavailable CCR4 antagonists(I), and their activity in in vitro and in vivo models, is described herein. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to antitumor ccr4 antagonists checkpoint inhibitors combination immune response bioavailability, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application In Synthesis of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

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

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