Category: 1211568-27-2

On April 30, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmermann, Kurt published a patent.Related Products of 1211568-27-2 The title of the patent was Bifunctional heterocycles, their use in targeted degradation of rapidly accelerated fibrosarcoma polypeptides and their preparation. And the patent contained the following:

The present disclosure relates bifunctional compounds of formula ULM-L-PTM, their use in modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein) and treatment of diseases that result from aggregation or accumulation of the target protein. and their preparation Compounds of formula ULM-L-PTM, wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. comprising a RAF protein targeting moiety; L is a bond or chem. linking moiety connecting ULM and PTM; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorph and prodrug thereof, are claimed. Compound I was prepared using a multistep procedure (procedure given). The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to bifunctional heterocycle preparation raf modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On November 9, 2021, Qin, Chong; Chen, Yiming; Zhong, Tengjiang; Zhang, Sai; Ge, Ling published a patent.Synthetic Route of 1211568-27-2 The title of the patent was High-efficiency androgen receptor modulator and its application. And the patent contained the following:

A high-efficiency androgen receptor modulator (e.g., I) having wide application in field of pharmaceuticals is provided. The androgen receptor (AR) modulator contains the E3 ubiquitin ligase ligand combined with an androgen receptor (AR) modulator. The androgen receptor (AR) modulators and their pharmaceutical composition are used in preparation of antiandrogen drugs. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Synthetic Route of 1211568-27-2

The Article related to heterocyclyl androgen receptor modulator antitumor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Synthetic Route of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On July 29, 2022, Zhang, Chen; Wang, Jianmin; Qian, Guofei; Huang, Zhenggang; Tang, Pingming; Ye, Fei; Li, Yao; Ni, Jia; Yan, Pangke published a patent.Application of 1211568-27-2 The title of the patent was Preparation of a bifunctional molecule with EGFR degradation as antitumor agent. And the patent contained the following:

The present invention discloses a preparation of a bifunctional mol. with EGFR degradation as antitumor agent, which can be used to prepare drugs for treating diseases related to EGFR activity. The invention compound was prepared via the reaction of benzyl piperazine-1-carboxylate and tert-Bu 3-oxoazetidine-1-carboxylate, followed by deprotection, condensation, reduction reaction and substitution reaction. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Application of 1211568-27-2

The Article related to preparation egfr degradation antitumor agent condensation suzuki coupling, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 22, 2020, Du, Wu; Wen, Kun; Fu, Yiwei; Lv, Haibin; He, Jinyun; Qin, Dekun; Li, Yu; Duan, Jingyi; Li, Yong; Ai, Chaowu; Tu, Zhilin; Chen, Yuanwei; Li, Xinghai published a patent.HPLC of Formula: 1211568-27-2 The title of the patent was A class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and application. And the patent contained the following:

The invention disclosed a class of bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and application. The claimed compound is shown in structure ARB-L-U (ARB = androgen receptor recognition/binding part; L = linker part; U = ubiquitin protease recognition/binding part). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The claimed compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).HPLC of Formula: 1211568-27-2

The Article related to bifunctional chimeric heterocycle preparation androgen receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Related Products of 1211568-27-2 The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Related Products of 1211568-27-2 The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On July 7, 2022, Huo, Changxin; Wang, Hexiang; Lv, Gang; Wang, Zhiwei; Liu, Huaqing published a patent.COA of Formula: C15H29N3O2 The title of the patent was Degradation of bruton’s tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use. And the patent contained the following:

Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. The title compounds I [ring A and B = (independently) an aromatic ring comprising 0-3 heteroatoms selected from N, S and O as ring member(s); Z1-Z4 = (independently) N or CRz; L = (independently) a bond, alkylene, O, etc.; m, n and q = (independently) 0-4; t = 0-2; R1 and R2 = (independently) H, alkyl, cycloalkyl, etc.; R3, R5 and R6 = (independently) H, halo, alkyl, etc.; Rz = the bond between moiety and Linker-Degron moiety, H, halo, etc.; the Linker = a bond or a divalent linking group; and the Degron = E3 Ubiquitin ligase moiety] or pharmaceutically acceptable salts thereof, were prepared E.g., a multi-step synthesis of II, starting from 4-phenoxybenzaldehyde and 4-methylbenzenesulfonohydrazide, was described. Exemplified compounds I were evaluated for their activity as BTK degradation (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2

The Article related to bifunctional compound preparation bruton’s tyrosine kinase btk degradation, targeted protein degrader btk e3 ubiquitin ligase bifunctional compound, btk inhibitor e3 ligase conjugation bifunctional compound preparation and other aspects.COA of Formula: C15H29N3O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 12, 2018, Crew, Andrew P.; Hornberger, Keith R.; Snyder, Lawrence B.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Crews, Craig M.; Dong, Hanqing published a patent.Category: piperazines The title of the patent was Preparation of bifunctional compounds for the targeted degradation of androgen receptor. And the patent contained the following:

The invention relates to bifunctional compounds, which find utility to degrade and (inhibit) androgen receptor. In particular, the invention is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds androgen receptor, such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of androgen receptor. The invention exhibits a broad range of pharmacol. activities associated with compounds according to the present invention, consistent with the degradation/inhibition of androgen receptor (data given). The invention compounds are claimed to be useful for the treatment of cancer or Kennedy’s disease, or both. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Category: piperazines

The Article related to protac modulator preparation targeted ubiquitination androgen receptor degradation inhibition, preparation bifunctional compound degradation androgen receptor, treatment cancer kennedy disease preparation bifunctional compound and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 10, 2019, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Berlin, Michael; Crews, Craig M. published a patent.SDS of cas: 1211568-27-2 The title of the patent was Preparation of bifunctional compounds as modulators of proteolysis useful for treating cancer. And the patent contained the following:

The present disclosure relates to bifunctional compounds ULM-L-PTM [the ULM = a small mol. E3 ubiquitin ligase binding moiety that binds an E3 ubiquitin ligase;the PTM = a small mol. comprising a Kirsten rat sarcoma protein (KRas) targeting moiety; the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins (IAP) 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, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Over 500 title compounds were prepared E.g., a multi-step synthesis of I, starting from 2,2,5-trimethyl-4-oxo-3,8,11-trioxa-5-azatridecan-13-yl 4-methylbenzenesulfonate and 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione, was described. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given for representative title compounds). Diseases or disorders that result from aggregation, accumulation, and/or overactivation 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 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).SDS of cas: 1211568-27-2

The Article related to bifunctional compound preparation kras modulator antitumor e3 ubiquitin ligase, von hippel lindau cereblon protein bifunctional compound preparation antitumor, apoptosis protein inhibitor antitumor bifunctional compound quinazolinamine preparation, mouse double minute 2 homolog mdm2 bifunctional compound preparation and other aspects.SDS of cas: 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On July 7, 2022, Huo, Changxin; Wang, Hexiang; Lv, Gang; Wang, Zhiwei; Liu, Huaqing published a patent.COA of Formula: C15H29N3O2 The title of the patent was Degradation of bruton’s tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use. And the patent contained the following:

Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. The title compounds I [ring A and B = (independently) an aromatic ring comprising 0-3 heteroatoms selected from N, S and O as ring member(s); Z1-Z4 = (independently) N or CRz; L = (independently) a bond, alkylene, O, etc.; m, n and q = (independently) 0-4; t = 0-2; R1 and R2 = (independently) H, alkyl, cycloalkyl, etc.; R3, R5 and R6 = (independently) H, halo, alkyl, etc.; Rz = the bond between moiety and Linker-Degron moiety, H, halo, etc.; the Linker = a bond or a divalent linking group; and the Degron = E3 Ubiquitin ligase moiety] or pharmaceutically acceptable salts thereof, were prepared E.g., a multi-step synthesis of II, starting from 4-phenoxybenzaldehyde and 4-methylbenzenesulfonohydrazide, was described. Exemplified compounds I were evaluated for their activity as BTK degradation (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2

The Article related to bifunctional compound preparation bruton’s tyrosine kinase btk degradation, targeted protein degrader btk e3 ubiquitin ligase bifunctional compound, btk inhibitor e3 ligase conjugation bifunctional compound preparation and other aspects.COA of Formula: C15H29N3O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics