Category: 1211568-27-2

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.Formula: C15H29N3O2 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 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Formula: C15H29N3O2

The Article related to polycyclic targeted protein kinase raf, Pharmaceuticals: Pharmaceutics and other aspects.Formula: C15H29N3O2

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

On January 27, 2022, Lee, Song Hee; Ryu, Je Ho; Ahn, Jung Min; Choi, Yu Ri; Lee, Ho Hyun; Jang, Mi Young; Woo, Yae Jin; Kim, Hanwool; Kim, Ji Young; Park, Ji Youn published a patent.Related Products of 1211568-27-2 The title of the patent was Amide compound for androgen receptor degradation, and pharmaceutical use thereof. And the patent contained the following:

The present invention provides a compound I [R1 = H, alkyl, halogen, etc.; R2 = H, alkyl, halogen, etc.; X1, X3, X4 and X5 = independently CH or N; X2 = CR3 or N; R3 = H, alkyl, halogen, etc.; n = 0, 1, or 2; m = 0 or 1; L = -(CH2)q1-A1-(CH2)q2-B1-(CH2)q3-A2-(CH2)q4-B2-(CH2)q5-A3-(CH2)q6-B3-; A1, A2 and A3 = independently direct bond, -O-, -N(R4)-, etc.; R4 = H, alkyl or haloalkyl; B1, B2 and B3 = independently direct bond, cycloalkyl, heterocycle, etc.; q1-q6 = independently 0-6; E = Q1 or Q2; X6, X7, X8 and X9 = independently CH or N; Y = -C(R6)2-, -C(O)-, -C(R6)2-C(R6′)2-, etc.; Z = direct bond, -C(R6)2-, -O-, etc.; R5 and R5′ = independently H, alkyl, halogen, etc.; R6 and R6′ = independently H, alkyl, halogen, etc.] of a specific chem. structure, having androgen receptor (AR) degradation activity, or a pharmaceutically acceptable salt thereof. The present invention also provides a composition containing the compound or a pharmaceutically acceptable salt thereof. According to present invention, provided is a pharmaceutical use of the compound, the salt thereof, and the composition containing same for treating or preventing AR-related diseases. According to the present invention, further provided is a method for treating or preventing AR-related diseases, the method comprising administering, to a subject in need of treatment, an effective amount of the compound, the salt thereof, or the composition containing same. For example, compound II (preparation given) was coupled with compound III (preparation given) to provide compound IV. 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 amide compound preparation androgen receptor degradation activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 1211568-27-2

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

On January 27, 2022, Lee, Song Hee; Ryu, Je Ho; Ahn, Jung Min; Choi, Yu Ri; Lee, Ho Hyun; Jang, Mi Young; Woo, Yae Jin; Kim, Hanwool; Kim, Ji Young; Park, Ji Youn published a patent.Related Products of 1211568-27-2 The title of the patent was Amide compound for androgen receptor degradation, and pharmaceutical use thereof. And the patent contained the following:

The present invention provides a compound I [R1 = H, alkyl, halogen, etc.; R2 = H, alkyl, halogen, etc.; X1, X3, X4 and X5 = independently CH or N; X2 = CR3 or N; R3 = H, alkyl, halogen, etc.; n = 0, 1, or 2; m = 0 or 1; L = -(CH2)q1-A1-(CH2)q2-B1-(CH2)q3-A2-(CH2)q4-B2-(CH2)q5-A3-(CH2)q6-B3-; A1, A2 and A3 = independently direct bond, -O-, -N(R4)-, etc.; R4 = H, alkyl or haloalkyl; B1, B2 and B3 = independently direct bond, cycloalkyl, heterocycle, etc.; q1-q6 = independently 0-6; E = Q1 or Q2; X6, X7, X8 and X9 = independently CH or N; Y = -C(R6)2-, -C(O)-, -C(R6)2-C(R6′)2-, etc.; Z = direct bond, -C(R6)2-, -O-, etc.; R5 and R5′ = independently H, alkyl, halogen, etc.; R6 and R6′ = independently H, alkyl, halogen, etc.] of a specific chem. structure, having androgen receptor (AR) degradation activity, or a pharmaceutically acceptable salt thereof. The present invention also provides a composition containing the compound or a pharmaceutically acceptable salt thereof. According to present invention, provided is a pharmaceutical use of the compound, the salt thereof, and the composition containing same for treating or preventing AR-related diseases. According to the present invention, further provided is a method for treating or preventing AR-related diseases, the method comprising administering, to a subject in need of treatment, an effective amount of the compound, the salt thereof, or the composition containing same. For example, compound II (preparation given) was coupled with compound III (preparation given) to provide compound IV. 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 amide compound preparation androgen receptor degradation activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 1211568-27-2

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

On April 22, 2021, Berlin, Michael; Dong, Hanqing; Sherman, Dan; Snyder, Lawrence; Wang, Jing; Zhang, Wei published a patent.COA of Formula: C15H29N3O2 The title of the patent was Bifunctional molecules containing an E3 ubiquitin ligase binding moiety linked to a BCL6 targeting moiety and their preparation. And the patent contained the following:

Bifunctional compounds of formula I, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. Bifunctional compounds of formula I wherein ULM is a small E3 ubiquitin ligase binding moiety that bonds Von Hippel-Lindau, cereblon; PTM is a small mol. comprising a B-cell lymphoma 6 protein targeting moiety; L is a bond and a chem. linker; pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, and polymorphs thereof, are claimed. The bifunctional compounds of the disclosure exhibit 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 are treated or prevented with compounds and compositions of the disclosure. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their BCL6 protein degradation activity (some data given). 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 mol preparation bcl6 protein degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

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

On October 8, 2020, Yang, Bin; Hayhow, Thomas George Christopher; Fallan, Charlene; Scott, James Stewart; Diene, Coura; Barlaam, Bernard Christophe; Nissink, Johannes Wilhelmus Maria published a patent.Application of 1211568-27-2 The title of the patent was Pyrimidinyltetrahydropyridoindoles as estrogen receptor degrading PROTACs and their preparation. And the patent contained the following:

The specification relates to compounds of formula I and pharmaceutically acceptable salts thereof. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them. Compounds of formula I wherein A and G are independently CR5 and N; E and Q are independently CH and N; R1 and R2 are H; R1R2 can be taken together to form oxo; R3 and R4 are independently H and OMe; R5 is H, F, Cl, CN, Me and OMe; R6 and R7 are independently H, Me and F; R6R7 can be taken together to form cyclopropyl and oxetanyl; R8 is H, Me, F, CH2F, CN, etc.; Linker is (un)substituted. (un)branched, (un)cyclized, (un)saturated 6 to 15 carbon atom moiety where 1 ot 6 carbon atoms may optionally be replaced with O, N and S; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen binding affinity and estrogen degradation activity. From the assay, it was determined that compound II exhibited IC50 values of 3.1 nM and 1.1 nM toward ER binding and ER degradation, resp. 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 pyrimidinylpyridoindole preparation er degrading protac, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1211568-27-2

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

On June 2, 2022, Zhang, Chen; Liao, Yuting; Ye, Fei; Tang, Pingming; Chen, Xiaogang; Lu, Yonghua; Gao, Qiu; Li, Yao; Ni, Jia; Yan, Pangke published a patent.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Benzene ring derivative, and composition and pharmaceutical use thereof. And the patent contained the following:

Disclosed are a compound or a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, and an intermediate thereof, and the use thereof in AR or AR splicing mutant-related diseases such as cancer. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to benzene ring derivative preparation treatment cancer disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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

On March 17, 2022, Ryu, Hyung-Chul; Kim, Jae-Sun; Lim, Jee-Woong; Lee, Ju Young; Choi, Kwanghyun; Rajesh, Rengasamy; Chang, Duk-Ho; Gwon, Hyeok Jun; Kang, Hyo Jin published a patent.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of pyrimidinamine derivatives for suppressing EGFR mutant cancer and pharmaceutical use thereof. And the patent contained the following:

The invention relates to pyrimidinamine derivatives of formula I, pharmaceutically acceptable salts, or pharmaceutical compositions thereof which have the activity of inhibiting and/or degrading mutant EGFR protein and are useful for the treatment or prevention of cancer with EGFR mutation, especially lung cancer. The present disclosure also provides a method for the treatment or prevention of EGFR mutation cancer, especially lung cancer, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing same to a subject in need of treatment. Compounds of formula I wherein R1 and R2 are independently H, (halo)alkyl, or trideuteromethyl; R3 – R6 are independently H, halo, cyano, (halo)alkyl, (halo)alkoxy, etc.; m and n are independently 0-4; A is heterocyclyl; L is a connecting group through covalent bond; B is Q1 or Q2; X is single bond, (CH2)1-6, O-(CH2)0-6, C(O)-(CH2)0-6, N(R13)-(CH2)0-6, C(O)-N(R13)-(CH2)0-6, N(R13)-C(O)-(CH2)0-6, etc.; W is C(R14)2 or C(O); R8 is H, hydroxy, halo, (halo)alkyl, or (halo)alkoxy; R9 and R10 are independently H or alkyl; R13 and R14 are independently H or alkyl; o and p are independently 1-3; Y is (halo)alkyl, aryl, etc.; Z is O or S; R11 is H, alkyl, or (CH2)1-6-C(O); R12 is H, alkyl, or cycloalkyl; are claimed. The invention compounds were evaluated for the EGFR protein degradation activity (biol. data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to pyrimidinamine derivative preparation egfr mutant lung cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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

On April 28, 2022, Berlin, Michael; Crew, Andrew; Dong, Hanqing; Hornberger, Keith; Snyder, Lawrence; Wang, Jing; Zimmermann, Kurt published a patent.Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of bifunctional compounds and methods for the targeted degradation of androgen receptor protein. And the patent contained the following:

Bifunctional compounds e.g. I, which find utility as modulators of androgen receptor (AR), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds AR, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. Example I was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their androgen receptor modulatory activity (some data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to bifunctional preparation targeted degradation androgen receptor modulator anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

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

On February 1, 2022, Zhang, Chen; Liao, Yuting; He, Ping; Chen, Xiaogang; Xuan, Zhaoli; Ye, Fei; Tang, Pingming; Wan, Songlin; Li, Yao; Ni, Jia; Yan, Pangke published a patent.COA of Formula: C15H29N3O2 The title of the patent was Preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. And the patent contained the following:

The present invention relates to preparation of BTK inhibitor cyclic derivative and its pharmaceutical application in treatment of BTK-related diseases. In particular, the BTK inhibitor ring derivative B-L-K (wherein, L = -Ak1-Cy1-Ak2-Cy2-Ak3-Cy3-Ak4-Cy4-Ak5-; Ak1 – Ak5 = CH2, O, -NRb0-, C=O, C=C or bond; Cy1 – Cy4 = optionally substituted 3-12 membered heterocycle, optionally substituted 3-12 membered cycloalkyl, optionally substituted 6-10 membered aryl, or bond; B = B1-W1-B2-B3-B4- or I, when B = B1-W1-B2-B3-B4-, Cy1, Cy2, Cy3, and Cy4 cannot be bonds at the same time; when B = B1-W1-B2-B3-B4-, and Ak1, Ak2, Ak3, Ak4 or Ak5 are not bonds, they cannot be directly connected to each other). Further, (B1 and B2 = optionally substituted 6-membered heteroaromatic ring or phenyl; W1 = -O-, -S-, -NH-, -NHCO- or -CONH-; B3 = optionally substituted heterocyclic ring; B4 = optionally substituted 4-7-membered monocycloalkyl, optionally substituted 6-12-membered spirocycloalkyl, optionally substituted 5-10-membered cycloalkyl derivative etc.; B5 or B6 = optionally substituted Ph or 5-6-membered heteroaryl; Rb6 = H, C1-4 alkyl, halogen-substituted C1-4 alkyl or hydroxy-substituted C1-4 alkyl; Rb7 and Rb8 = H, F, Cl, Br, I, OH, NH2, CN, CF3, -C(=O)NH2 etc.; m = 0, 1 or 2; K = heterocyclic group, cycloalkyl carbonyl-group, aralkyl carbonyl-group etc.) or stereoisomer, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof were prepared The inventive BTK inhibitor cyclic derivatives are useful for treating BTK-related diseases such as tumors or autoimmune system diseases. 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 azaheterocyclic compound preparation btk inhibitor antitumor autoimmune disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

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

On April 22, 2021, Berlin, Michael; Dong, Hanqing; Sherman, Dan; Snyder, Lawrence; Wang, Jing; Zhang, Wei published a patent.COA of Formula: C15H29N3O2 The title of the patent was Bifunctional molecules containing an E3 ubiquitin ligase binding moiety linked to a BCL6 targeting moiety and their preparation. And the patent contained the following:

Bifunctional compounds of formula I, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. Bifunctional compounds of formula I wherein ULM is a small E3 ubiquitin ligase binding moiety that bonds Von Hippel-Lindau, cereblon; PTM is a small mol. comprising a B-cell lymphoma 6 protein targeting moiety; L is a bond and a chem. linker; pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, and polymorphs thereof, are claimed. The bifunctional compounds of the disclosure exhibit 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 are treated or prevented with compounds and compositions of the disclosure. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their BCL6 protein degradation activity (some data given). 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 mol preparation bcl6 protein degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

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